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Recent progress towards transition-metal-catalyzed direct arylation of heteroarenes
Yexiang Su, Li-Ping Sun
[Abstract] [Purchase Article] [BSP/MROC/E-Pub/00001]


“In water” synthesis of heterocyclic compounds
Siva S. Panda and Subhash C. Jain
[Abstract] [Purchase Article] [BSP/MROC/E-Pub/00003]


Some Recent Topics in Cigarette Smoke Science
C. Liu, K.G. McAdam and T.A. Perfetti
[Abstract] [Purchase Article] [BSP/MROC/E-Pub/00004]


Microwave Photochemistry. Applications in Organic Synthesis
Vladimír Církva and Stanislav Relich
[Abstract] [FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00005]


Free Radicals in Tobacco Smoke
Barry Dellinger, Lavrent Khachatryan, Sofia Masko, Slawomir Lomnicki
[Abstract] [Purchase Article] [BSP/MROC/E-Pub/00006]


The role of oxidative stress in smoking related diseases
Ian M. Fearon, Gary Phillips, Tony Carr, Mark Taylor, Damien Breheny & Stephen P. Faux
[Abstract] [Purchase Article] [BSP/MROC/E-Pub/00008]


The Reactivity of Free Radicals in Biomass Char Studied by EPR Spectroscopy
Xiuzhi Gao and Jiwen Feng
[Abstract] [Purchase Article] [BSP/MROC/E-Pub/00009]


Copper-Catalyzed Direct Amination of Halo(hetero)arenes With Sodium Azide As The Amino Source
S. Messaoudi, J.-D. Brion and M. Alami
[Abstract] [Purchase Article] [BSP/MROC/E-Pub/00013]


A Novel Mechanism for Metal-independent Hydroxyl Radical Production by Hydrogen Peroxide and Halogenated Quinones
Ben-Zhan Zhu, Rui-Mei Fan and Na Qu
[Abstract] [Purchase Article] [BSP/MROC/E-Pub/00017]


Methods for Analysis of Free Radicals in Cigarette Smoke
E.A. Robinson and J.D. Johnson
[Abstract] [Purchase Article] [BSP/MROC/E-Pub/00018]


Oxygen Free Radicals and Its Biomedical Implications: A Mini Review
R. N. Sharan, M. M. Odyuo and S. Purkayastha
[Abstract] [Purchase Article] [BSP/MROC/E-Pub/00019]


Mechanism of oxidative broncho-epithelial cell damage with reference to gas phase cigarette smoke
John C. Stavridis and George E. Baltatzis
[Abstract] [FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00023]


Hydrogen Peroxide Derived from Cigarette Smoke: "Pardon impossible, to be sent to Siberia"?
Valery A. Menshov and Alexey V. Trofimov
[Abstract] [Purchase Article] [BSP/MROC/E-Pub/00024]


Gas-Phase Radicals in Cigarette Smoke: A Re-evaluation of the Steady-State Model and the Cambridge Filter Pad
Jan B. Wooten
[Abstract] [Purchase Article] [BSP/MROC/E-Pub/00026]


Biomarkers Of Oxidative Stress And The Relationship To Cigarette Smoking
F.J. Lowe and E. Cemeli
[Abstract] [Purchase Article] [BSP/MROC/E-Pub/00027]


Microwave Assisted Synthesis of Imidazoles - A Review
Girish Kumar Gupta, Nidhi Rani and Vinod Kumar
[Abstract] [FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00028]


Chemistry and Biological Activities of 1,3-Benzothiazoles
Victor Facchinetti, Raísa da R. Reis, Claudia R.B. Gomes and Thatyana R.A. Vasconcelos
[Abstract] [FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00029]


Ionic liquids: a new strategy in pharmaceutical synthesis
Tomasz Siódmiak, Michał Piotr Marszałł and Anna Proszowska
[Abstract] [FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00030]


Recent Development in Aerobic Oxidation of Amines
Bo-Tao Xin, Qing-Fa Zhou and Tao Lu
[Abstract] [FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00031]


Bioorganic compounds produced by the fungus Monascus and their use in health sciences and medicine
Megumi Kuba-Miyara and Masaaki Yasuda
[Abstract] [FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00032]


Labdane diterpenes with highly functionalised B rings
I. S. Marcos, L. Castañeda, P. Basabe, D. Díez and J. G. Urones
[Abstract] [FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00033]


Penetration of infectious prion protein in the intestine during the lactation period
Ryuta Uraki, Akikazu Sakudo, Yasuhisa Ano, Juri Kono, Masayoshi Yukawa, Gianluigi Zanusso Antonio Toniolo and Takashi Onodera
[Abstract] [FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00034]


Recent Advances in the Development of Small-Molecule Compounds Targeting HIV-1 gp41 as Membrane Fusion Inhibitors
Norihito Kawashita, Yu-Shi Tian, U. Chandimal de Silva, Kousuke Okamoto and Tatsuya Takagi
[Abstract] [FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00035]


Recent Applications of the Simple Hydrocarbon Cyclooctatetrene as a Starting Material for Complex Molecule Synthesis
Kevin W. Glaeske and William A. Donaldson
[Abstract] [FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00036]


Chromogenic Sensors for Anionic Species Based on Indicator Displacement Approach
Kai Liu, Xiumei Su and Jianzhong Huo
[Abstract] [FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00037]


Recent Developments in Anti-influenza A Virus Drugs and Use in Combination Therapies
Kunihiro Kaihatsu, and Dale L. Barnard
[Abstract] [FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00038]


Review On Synthesis Of Biologically Active Diazepam Derivatives
S. Sathish Kumar, Helen P. Kavitha, S. Arulmurugan and B.R. Venkatraman
[Abstract] [FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00039]


Synthesis of Different classes of Five / Five Membered Heterocyclic Cyanine Dyes: A Review Paper
H.A. Shindy
[Abstract] [FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00040]


Synthesis and Application of Metal Ion Containing Ionic Liquids: A Brief Review
Li-Juan Wang and Cui-Qua Lin
[Abstract] [FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00041]



Abstracts



Recent progress towards transition-metal-catalyzed direct arylation of heteroarenes
Yexiang Su, Li-Ping Sun
[Purchase Article] [BSP/MROC/E-Pub/00007]

In this short review, the direct intermolecular cross-coupling reactions of heteroarenes with aryl (pseudo)halides catalyzed by transition metals via C-H bond cleavage in recent years are depicted. The fundamental emphasis has been given to the synthetic aspects of different intermolecular direct cross-coupling reaction. Many of the attention are drawn to the palladium-catalyzed arylation reactions due to its predominant utility at present. Meanwhile, the procedures employed other transition metals are also presented.
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“In water” synthesis of heterocyclic compounds
Siva S. Panda and Subhash C. Jain
[Purchase Article] [BSP/MROC/E-Pub/00003]

Recently the aqueous medium has attracted the interest of organic chemists, and many, sometimes surprising, discoveries have been made. Among the organic reactions investigated in aqueous medium, the synthesis of heterocyclic compounds has been the most widely studied because heterocyclic compounds are rich sources of diverse physical, chemical, and biological properties. They are commonly used as templates to design biologically active agents in medicinal chemistry. Moreover, in the past 20 years, the drug-discovery process has undergone extraordinary changes, and high-throughput biological screening of potential drug candidates has led to an ever-increasing demand for novel drug-like compounds.  Noteworthy advantages were observed during the course of our study on “in water” synthesis of heterocyclic compounds. The established advantages of water as a solvent for reactions are, water is the most abundant and available resource on the planet and many biochemical processes occur in aqueous medium. This review will focus on describing new developments in the application of water in the organic synthesis of heterocycles. Heterocycles that will be covered include acridine, benzothiazole, benzopyran, isoxazole, pyradazine, pyrazole, pyridine, pyrimidine, pyrrole, quinazoline, quinoline, quinoxaline, thiadiazole, triazole, xanthene, xanthone and others.
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Some Recent Topics in Cigarette Smoke Science
C. Liu, K.G. McAdam and T.A. Perfetti
[Purchase Article] [BSP/MROC/E-Pub/00004]

This short review covered some fundamental aspects of cigarette combustion and smoke formation processes, including how cigarettes burn, how smoke is formed and transferred, and the complexity of cigarette smoke composition. Particular emphasis has been placed on recent progress in understanding on the generation and measurement of cigarette smoke, the use of techniques which reproduce the basic combustion phenomena of a burning cigarette, and the highly sensitive nature of the physico-chemical reactions behind smoke formation as a result of puffing parameters employed. Examples are given to demonstrate that the sampling and measurement techniques employed must preserve the true chemical nature of the species under investigation.This is particularly important for highly reactive species such as free radicals. Ultimately, it is essential to standardise different smoke analysis procedures between different laboratories to provide a consistent basis for scientific and regulatory consideration.
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Microwave Photochemistry. Applications in Organic Synthesis
Vladimír Církva and Stanislav Relich
[FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00005]

This review article is the second of the comprehensive series on survey of the microwave photochemical and photocatalytic processes, and is focused specially on the microwave-assisted photochemical applications of the electrodeless discharge lamps (EDLs) in organic synthesis. The concept of microwave organic photochemistry is an important issue in synthetic chemistry and material science, and is presented in several schemes. Likewise, the various microwave photochemical reactor types (batch with external or internal light source, flow-through with external light source, annular flow-through with internal EDL, cylindrical flow-through surrounded with EDL, and mixed flow-through with internal EDL) with different arrangement of the lamps are described.
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Free Radicals in Tobacco Smoke
Barry Dellinger, Lavrent Khachatryan, Sofia Masko, Slawomir Lomnicki
[Purchase Article] [BSP/MROC/E-Pub/00006]

A critical examination of the literature on gas-phase free radicals and TPM-associated EPFRs in cigarette smoke is presented.  These radicals participate in catalytic cycles that generate ROS that can result in oxidative stress.  It seems that primary radicals originate from the direct decomposition of tobacco constituents are linked to the chemical structure of the constituents and the temperature of pyrolysis.  On the other hand, secondary radicals are generated during aging of smoke.  Their EPR spectra are indicative of hydroquinone and catechol. Lignin, chlorogenic acid, and proteins are major precursors of EPFRs in TPM, but combinations of components form more secondary radicals than the sum of the individual components suggesting a synergistic role of TPM in the formation and the stabilization of secondary radicals. Matrix isolation EPR has identified cyclopentadienyl, phenoxyl, and semiquinone radicals as additional free radicals formed from phenolic precursors that may be responsible for gas-phase alkoxy radicals previously identified using spin-trapping techniques. EPFRs are found to initiate catalytic cycles that generate ROS and the overall concentrations of ROS generated by EPFRS are expected to be much higher than that generated by hydroquinones/quinones.
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The role of oxidative stress in smoking related diseases
Ian M. Fearon, Gary Phillips, Tony Carr, Mark Taylor, Damien Breheny & Stephen P. Faux
[Purchase Article] [BSP/MROC/E-Pub/00008]

Oxidative stress, the accumulation of oxygen free radicals (reactive oxygen species) above and beyond the capacity of a cell to utilise antioxidant systems to detoxify these potentially damaging molecules, is a common feature of many human disorders. Cigarette smoke is not only a source of free radicals but is also a potent stimulator of the intracellular production of free radicals, by the mitochondrial electron transport chain and the plasmalemmal NADPH oxidase. Adding to this free radical burden is the reduction, by cigarette smoke, of the cellular antioxidant capacity. Together, the increased production and reduced detoxification of free radicals has been strongly linked to smoking-induced diseases including atherosclerotic cardiovascular disease, cancer and chronic obstructive pulmonary disease (COPD). In this review, we discuss the mechanisms underlying cellular free radical production, relate this to the three major smoking-related human diseases listed above and present potential mechanisms by which cigarette smoke may increase the oxidative burden on cells and contribute to disease.
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The Reactivity of Free Radicals in Biomass Char Studied by EPR Spectroscopy
Xiuzhi Gao and Jiwen Feng
[Purchase Article] [BSP/MROC/E-Pub/00009]

In this review, the features of electron paramagnetic (EPR) spectra of biomass chars prepared from single biopolymers (cellulose, pectin, lignin, etc.) to complex plant materials (tobacco) are summarized, and the interaction of biomass chars with air, O₂ and/or H₂O as detected by EPR is critically examined. The effects of inorganic components are emphasized for understanding the creation and annihilation of free radicals in biomass chars in the presence of O₂ or air. While the EPR spectra can be difficult to interpret, the interactions observed reflect fundamental processes occurring in biomass chars during pyrolysis and combustion that may affect the chemical composition of biomass conversion products as well as cigarette emission.
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Copper-Catalyzed Direct Amination of Halo(hetero)arenes With Sodium Azide As The Amino Source
S. Messaoudi, J.-D. Brion and M. Alami
[Purchase Article] [BSP/MROC/E-Pub/00013]

In the synthesis of primary (hetero)aryl amines through copper-catalysis, the ammonia surrogates or aqueous ammonia nucleophilic partners can be replaced by sodium azide. Recent efforts in copper-mediated transformation of (hetero)aryl halides to (hetero)aryl amines using azide anion as the amino source are discussed in this highlights.
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A Novel Mechanism for Metal-independent Hydroxyl Radical Production by Hydrogen Peroxide and Halogenated Quinones
Ben-Zhan Zhu, Rui-Mei Fan and Na Qu
[Purchase Article] [BSP/MROC/E-Pub/00017]

The hydroxyl radical (•OH) has been considered to be one of the most reactive oxygen species that are produced in biological systems. Frequently, •OH formation is ascribed to the transition metal-catalyzed Fenton reaction. During the study of the molecular mechanism for the genotoxicity of the wood preservative pentachlorophenol (PCP), we found that •OH could be produced by H₂O₂ and PCP metabolite tetrachloro-1,4-benzoquinone (TCBQ) independent of transition metal ions. Further studies showed that TCBQ, but not its corresponding semiquinone radical, is essential for •OH production. Metal-independent production of ·OH could also be observed with other halogenated quinones and H₂O₂. Based on these data, we propose that •OH production by TCBQ and H₂O₂ is not through a semiquinone-dependent organic Fenton reaction, but rather through a novel nucleophilic substitution and homolytical decomposition mechanism. This represents a novel mechanism for •OH production not requiring the catalysis of redox-active transition metal ions, and may partly explain the potential carcinogenicity of the widely used biocides such as PCP and other polyhalogenated aromatic compounds.
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Methods for Analysis of Free Radicals in Cigarette Smoke
E.A. Robinson and J.D. Johnson
[Purchase Article] [BSP/MROC/E-Pub/00018]

Free radicals in the particulate phase of cigarette smoke were first measured by direct electron paramagnetic resonance (EPR) spectroscopy over 60 years ago.  Early efforts to measure free radicals in cigarette smoke were prompted by the theory that radicals could be involved in carcinogenesis.   It was thought that free radicals could be either direct acting or produced by other components of cigarette smoke such as polycyclic aromatic hydrocarbons.  Even today, it is uncertain which of these routes of action is the most important.  Ultimately, the development of a strategy to minimize potential biological damage from free radicals is dependent on the extent to which free radicals delivered in cigarette smoke are directly involved in disease processes.  In recent years, the primary instrumental means for identifying and studying free radicals in smoke have been both EPR and mass spectrometry (MS) techniques using spin trapping.  The spin trapping technique allows stabilization of short-lived species.  When coupled with MS, spin trapping allows complete structural characterization of free radicals.  When coupled with EPR, spin trapping allows structural characterization by comparison to EPR spectra of known chemical species.   Advances in the development of spin traps and spin trapping techniques, along with EPR and MS methods used for the study of cigarette smoke free radicals are presented in this review.
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Oxygen Free Radicals and Its Biomedical Implications: A Mini Review
R. N. Sharan, M. M. Odyuo and S. Purkayastha
[Purchase Article] [BSP/MROC/E-Pub/00019]

Free radicals (FR) are chemical species of significant importance to biological systems. FRs are generated by endo- as well as exogenous factors. Biological systems are equipped with appropriate metabolic pathways to remove cellular FR as well as repair the damages caused by them. Their cellular/physiological load profoundly influences the metabolism, physiology and overall well being of biological systems. Therefore, they are implicated in cellular degenerative processes and in patho-physiology, including carcinogenesis and ageing. The review shall attempt to give a generalized overview of FR chemistry, especially to the biologically important oxygen free radials (OFR) and reactive oxygen species (ROS). The review shall also discus the OFR/ROS biology to get an overview of the induced damage at molecular, cellular and organismal levels in order to give a perspective of their influences on the genomic integrity, cellular microenvironment and physiology with special reference to human health.
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Mechanism of oxidative broncho-epithelial cell damage with reference to gas phase cigarette smoke
John C. Stavridis and George E. Baltatzis
[FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00023]

Tobacco smoke contains many thousands of chemicals including a large number of carcinogens. The exposure of human tissues and organs to these carcinogens and their metabolism in relation to smoking-related cancer has been reviewed. The assault on DNA and RNA as well as other cellular components by the ROS is the base for oxidation. Free radicals (ROS) are implicated in chemical carcinogenesis via various metabolic pathways. The participation of free radicals in tobacco smoke in the process of carcinogenesis is mainly due to the effect of oxidative substances on the signal transduction pathways which lead to the cell replication by transforming the signaling proteins. However, the exact mechanism through which free radicals function in this process is not completely understood.
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Hydrogen Peroxide Derived from Cigarette Smoke: "Pardon impossible, to be sent to Siberia"?
Valery A. Menshov and Alexey V. Trofimov
[Purchase Article] [BSP/MROC/E-Pub/00024]

Hydrogen peroxide (H₂O₂) is one of the most important constituents in the metabolic chain transforming cigarette smoke in the human organism. The present analytical review provides a survey of the state-of-art in the study of H₂O₂ chemistry and biochemistry (both as a reactive and signaling species) in the context of cigarette smoking, taking into account both endogenous and exogenous (environmental, dietary, etc.) sources of H₂O₂. Particular attention is given to the methodological problems of monitoring smoke-associated H₂O₂. Our analysis is of prime interest for understanding the various mechanisms of smoke-induced oxidative stress and for developing rational approaches for diminishing the risk factors for human health associated with cigarette smoking.
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Gas-Phase Radicals in Cigarette Smoke: A Re-evaluation of the Steady-State Model and the Cambridge Filter Pad
Jan B. Wooten
[Purchase Article] [BSP/MROC/E-Pub/00026]

Cigarette smoke free radicals have been the subject of many years of investigation.  Recently, individual acyl and carbamoyl radicals in fresh whole cigarette smoke were isolated, identified, and quantified by HPLC-mass spectrometry for the first time.  These carbon-centered radicals do not conform to the established “steady-state model” for radical formation in gas-phase cigarette smoke.  In separate studies, NO₂ in fresh whole mainstream smoke has been measured on a puff-to-puff basis by highly precise and rapid tunable infrared diode laser spectroscopy (TILDAS).  Only the first puff contained a significant amount of NO₂ and its overall yield was substantially lower than previously reported.  Nevertheless, when the smoke was passed through a Cambridge filter pad, NO₂ appeared in the filtered gas-phase smoke during every puff, suggesting that NO₂ forms directly on the pad.  For fresh smoke, these results also challenge the applicability of the steady-state mechanism, which postulates that NO₂ in the smoke itself is an essential intermediate for gas-phase radical formation.  In this review, the historical investigations of cigarette smoke radicals are re-examined and the implications of the new spectroscopic and radical trapping data are discussed. Possible alternative mechanisms for radical formation in cigarette smoke are proposed.  When combined with data from previous corroborating reports, these recent results raise serious issues about the use of the Cambridge pad, which is conventionally used to separate gas smoke constituents from whole smoke, but may introduce more artifacts of measurement for certain reactive smoke constituents than previously appreciated.
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Biomarkers Of Oxidative Stress And The Relationship To Cigarette Smoking
F.J. Lowe and E. Cemeli
[Purchase Article] [BSP/MROC/E-Pub/00027]

Oxidative stress has been implicated in the development of smoking-related diseases such as lung cancer, cardiovascular disease and chronic obstructive pulmonary disease.  Damage to biological tissues from interactions with free radicals found within the smoke and induced within cells by smoke exposure,  is thought to contribute to smoking-related disease development.  Many of these radical components are very short-lived in vivo due to their highly reactive nature and the highly efficient detoxification mechanisms possessed by the body to counteract their effects.  Hence, biomarkers are needed to assess the extent of radical exposure and subsequent oxidative damage in humans.  Oxidised lipids, proteins and DNA bases persist longer in vivo, and have been extensively investigated as surrogate measures of radical damage.  Furthermore, assessment of the body’s antioxidant defence mechanisms such as antioxidant enzyme activity and antioxidant compounds can help to understand the extent of radical exposure.  This mini review critically evaluates various biomarkers falling into these categories and the consistency of their relationship with smoking status, as a preliminary evaluation of their usefulness in dissecting disease pathways in smokers.  The future use of such biomarkers is also briefly discussed.
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Microwave Assisted Synthesis of Imidazoles - A Review
Girish Kumar Gupta, Nidhi Rani and Vinod Kumar
[FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00028]

Imidazoles constitute a major class of five membered heterocylic compounds and have been found to be an integral part of many important pharmacological active compounds in the field of medicinal chemistry. Imidazoles are also of general synthetic utility since they permit functional group and structural modifications to synthesize number of substituted heterocycles. In literature various conventional methods are reported for the synthesis of imidazoles. Microwave assisted synthesis has become useful technique to medicinal chemists for rapid organic synthesis to avoid formation of side product. This review concludes various existing synthetic methods of imidazoles particularly focusing microwave assisted approach developed upto 2011.
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Chemistry and Biological Activities of 1,3-Benzothiazoles
Victor Facchinetti, Raísa da R. Reis, Claudia R.B. Gomes and Thatyana R.A. Vasconcelos
[FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00029]

Benzothiazoles and its derivatives are an important group of heterocyclic compounds that exhibit a wide range of pharmacological properties such as antitumor, antimicrobial, antidiabetic, anticonvulsant and anti-inflammatory. These different biological applications for benzothiazole compounds have motivated new efforts in search for novel derivatives with improved biological activity and diverse applications in pharmaceutical industry. Owing to the importance of this system, the aim of this review is to highlight aspects reported on the chemistry and biological activity of benzothiazoles during the past few years (2000-2010).
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Ionic liquids: a new strategy in pharmaceutical synthesis
Tomasz Siódmiak, Michał Piotr Marszałł and Anna Proszowska
[FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00030]

The industrial synthesis of pharmaceutical compounds often involves the use of organic solvents. Unfortunately, these reaction media are responsible for organic contaminations in the final product. In recent years, ionic liquids (ILs) have become the “green alternatives” of volatile organic solvents. Thus, the application of ILs instead of conventional reagents offer a new opportunity to solve problems of environmentally harmful solvents. This mini-review discusses a new application of ILs in laboratory-scale pharmaceutical synthesis.
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Recent Development in Aerobic Oxidation of Amines
Bo-Tao Xin, Qing-Fa Zhou and Tao Lu
[FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00031]

This review describes recent development in the aerobic oxidation of amines. A variety of ruthenium catalysts have shown excellent activity for the aerobic oxidation of amines. Several gold and copper catalysts are also effective for this reaction. Other metal-containing complexes are revealed to be active catalysts and an enzyme is also investigated for this oxidation. Meanwhile, various supports have been explored for this reaction and the availability of various supports with differing physical properties allows chemists to design and create many catalytic systems.
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Bioorganic compounds produced by the fungus Monascus and their use in health sciences and medicine
Megumi Kuba-Miyara and Masaaki Yasuda
[FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00032]

The filamentous fungus ‘Monascus’ has been used as a natural food coloring and folk medicine in East Asia for centuries. Several bioactive substances produced by Monascus species have been isolated and identified. Recent studies demonstrated their mode of action in vitro and effectiveness in vivo, and their utilization for health foods and medicine has advanced. This mini review will introduce the physiological functions and safety of bioorganic chemicals produced by Monascus species.
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Labdane diterpenes with highly functionalised B rings
I. S. Marcos, L. Castañeda, P. Basabe, D. Díez and J. G. Urones
[FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00033]

In this paper are presented a serie of labdanes diterpenes with highly functionalized B rings and natural origin, reported to date. In this review are shown the natural source, the structure, the biological activities and the synthesis of these compounds, described to date. The structures for these compounds have been clasified taking into account the number of oxygenated positions of the B ring. In this manner the classification has 7 groups of dioxygenated labdanes, 6 of trioxygenated and one group of the tetraoxygenated ones.
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Penetration of infectious prion protein in the intestine during the lactation period
Ryuta Uraki, Akikazu Sakudo, Yasuhisa Ano, Juri Kono, Masayoshi Yukawa, Gianluigi Zanusso Antonio Toniolo and Takashi Onodera
[FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00034]

Prion diseases are fatal neurodegenerative zoonotic foodborne disorders, which are caused by an abnormal isoform of prion protein (PrP^Sc) derived from the cellular isoform of prion protein (PrP^C). According to epidemiological surveillance and in vivo experiments, exposure to the PrP^Sc during the weaning period is fraught with risk, suggesting that, during development, the intestinal defenses and the immune system are involved in PrP^Sc infection susceptibility. Although it remains unclear how PrP^Sc passes through the natural biological barriers during its invasion of intestinal cells, the 37 kDa/67 kDa laminin receptor is suspected to be one of the receptors involved in PrP^Sc-incorporation. In addition, we have recently shown that the neonatal Fc receptor (nFcR), which contributes to the uptake of maternal antibodies into the intestine, may play an important role in PrPSc incorporation. In this review, recent studies on PrP^Sc uptake and models of PrP^Sc incorporation into the intestine via the laminin and Fc receptors are described.
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Recent Advances in the Development of Small-Molecule Compounds Targeting HIV-1 gp41 as Membrane Fusion Inhibitors
Norihito Kawashita, Yu-Shi Tian, U. Chandimal de Silva, Kousuke Okamoto and Tatsuya Takagi
[FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00035]

Over the past few years, remarkable progress has been made in the development of human immunodeficiency virus (HIV) membrane fusion inhibitors. The focus has been on peptide inhibitors, which were developed by mimicking HIV sequences; however, these types of inhibitors generally lack oral bioavailability and are expensive. Therefore, development of small-molecule inhibitors has gained importance and recently progressed. This paper reviews the rapid advancements in the development of small-molecule HIV inhibitors over the last decade.International Immunology Frontier Research Centre, Osaka University, Osaka 565-0871, Japan.
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Recent Applications of the Simple Hydrocarbon Cyclooctatetrene as a Starting Material for Complex Molecule Synthesis
Kevin W. Glaeske and William A. Donaldson
[FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00036]

Cyclooctatetraene [COT], a simple non-aromatic cyclic polyene, is capable of undergoing a variety of oxidation and cycloaddition reactions to afford polycyclic structures.  In addition, complexation of COT or the cycloaddition products with transition metals facilitates bond formation.  Recent developments in the reactivity of COT and application to the synthesis of naturally occurring and non-naturally occurring compounds is reviewed.
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Chromogenic Sensors for Anionic Species Based on Indicator Displacement Approach
Kai Liu, Xiumei Su and Jianzhong Huo
[FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00037]

This review describes some developments on the anion sensing based on the indicator displacement. The reported systems are mainly from 2006. The simple IDAs approach, as a useful and facile technique for the creation of optical sensors, would give rise to much more attention and is destined to flourish in future.
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Recent Developments in Anti-influenza A Virus Drugs and Use in Combination Therapies
Kunihiro Kaihatsu, and Dale L. Barnard
[FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00038]

The pandemic potential of influenza viruses has engaged a large portion of the antiviral drug discovery research community in the development of numerous antiviral agents, with the ultimate goal to supplement effective immunization when new strains arise, especially after an antigenic shift. Antiviral agents against influenza A targets different replication steps of the virus life cycles. Some of the agents are analogues of biomolecules required during virus infection and others are inspired from natural plant extracts. In this review, we summarize their mechanisms of action during the influenza life cycle in vitro and the efficacies of combinational therapies with these agents against the influenza virus infections in vivo.
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Review On Synthesis Of Biologically Active Diazepam Derivatives
S. Sathish Kumar, Helen P. Kavitha, S. Arulmurugan and B.R. Venkatraman
[Abstract] [FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00039]

The pharmacological importance of substituted 1,4-and 1,5-benzodiazepines have been well established and some derivatives are known as anxiolytic, anticonvulsant, hypnotic and anticancer agents. In recent years, much effort has been taken in the benzodiazepine area to develop new members of this family. This review focuses on the synthesis and the biological activities of benzodiazepam derivatives.
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Synthesis of Different classes of Five / Five Membered Heterocyclic Cyanine Dyes: A Review Paper
H.A. Shindy
[FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00040]

The paper is reviewing synthesis of different classes of biheterocyclic five/five membered cyanine dyes. In this paper review detailed synthesis steps for some of the biheterocyclic five/five membered cyanine dyes were represented by equations. The synthesis covers, monomethine cyanine dyes (simple cyanine dyes), aza-monomethine cyanine dyes, dimethine cyanine dyes, trimethine cyanine dyes (carbocyanine dyes), aza-trimethine cyanine dyes, tetramethine cyanine dyes, heptamethine  cyanine dyes (tricarbocyanine dyes), styryl cyanine dyes (hemi cyanine dyes), aza-styryl cyanine dyes (aza-hemi cyanine dyes) and apocyanine dyes. In addition, in the introduction section of this paper we shed some light on the uses and applications of cyanine dyes.
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Synthesis and Application of Metal Ion Containing Ionic Liquids: A Brief Review
Li-Juan Wang and Cui-Qua Lin
[FULL-TEXT INQUIRY] [BSP/MROC/E-Pub/00041]

Some recent developments concerning the syntheses, physical properties and application of metal ion containing ionic liquids (ILs) with magnetic behavior are highlighted. The component ions used so far include both inorganic and organic types, and various strategies, namely not only the proper choice but also the synthesis of anions to introduce the functionality, are presented.
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