<![CDATA[Current Organic Synthesis (Volume 21 - Issue 6)]]> https://www.benthamscience.com/journal/34 RSS Feed for Journals | BenthamScience EurekaSelect (+https://www.benthamscience.com) 2024-03-12 <![CDATA[Current Organic Synthesis (Volume 21 - Issue 6)]]> https://www.benthamscience.com/journal/34 <![CDATA[Pictet-Spengler Synthesis of N-heteroaromatics Extended Porphyrins]]>https://www.benthamscience.com/article/1328632024-03-12 Background: Porphyrins are highly conjugated heterocyclic compounds and are found as the backbone of many natural products such as heme and chlorophyll. To improve its biological and optical properties, the functionalization of porphyrin at its β- and meso-position has gained importance in recent years.

Objective: The purpose of this review is to describe the Pictet-Spengler method for the incorporation of nitrogenous and biologically important heterocyclic scaffolds such as pyrrolo-/indolo[1,2-a]quinoxaline, pyrrolo[1,2-a]pyrazine, and quinoline at the β- and meso-positions of the porphyrins to increase π-conjugation and improve their biological, optical, and electrochemical properties.

Conclusion: This review provides a comprehensive overview of the synthesis of N-heterocyclic ex-tended porphyrins and metalloporphyrins via a modified Pictet-Spengler approach. The synthesized porphyrins were found to be highly conjugated and exhibited improved photophysical properties com-pared to their parent analogues. Moreover, the review article provided a brief overview of the Pictet-Spengler procedure, including product yields, reaction conditions, photophysical properties of the synthesized products, and potential applications in a variety of fields.

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<![CDATA[Functionalized Morpholine-thiazole Scaffold: Synthetic Strategies and Applications]]>https://www.benthamscience.com/article/1330642024-03-12 <![CDATA[Transition Metals Catalyzed Direct C-H Chalcogentaion of Arenes and Heteroarenes]]>https://www.benthamscience.com/article/1313272024-03-12etc. have been extensively studied. Aromatic arenes owning bearing suitable directing groups appeared as the most promising coupling partners to selectively synthesize differently substituted aryl sulfones and aryl sulfides/selenides. The synthetic strategies were highly convenient owing to the regioselectivity of products, broad substrate scope, mild reaction conditions and excellent functional group tolerance. The current review article comprehensively summarizes the extent of C-S/Se bond formation via transition metal-catalyzed C-H bond activation with the assistance of directing groups to govern the site selectivity.]]> <![CDATA[Synthesis, Characterization, DPPH Radical Scavenging, Urease Enzyme Inhibition, Molecular Docking Simulation, and DFT Analysis of Imine Derivatives of 4-formylpyridine with Selective Detection of Cu<sup>+2</sup> Ions]]>https://www.benthamscience.com/article/1330852024-03-121H-NMR), ultraviolet-visible (UV-Vis) and Fourier transform infrared (FTIR) spectroscopy were utilized for the characterization. The chemosensing properties of [4((2-phenyl hydrazono)methyl) pyridine] (1), [2-(2-(pyridin-4-ylmethylene)hydrazinyl) pyridine] (2), and [4-methoxy-N-yl methylene) aniline] (3) imino bases have been explored for the first time in aqueous media. The photophysical properties of chemosensors (1, 2, and 3) were examined by various cations (Na+, NH4+, Ba+2, Ni+2, Ca+2, Hg+2, Cu+2, Mg+2, Mn+2, and Pd+2). The chemosensor (1) showed very selective binding capability with copper ions at low concentrations (20 μM) without the influence of any other mentioned ions. The maximum complexation was noted with Cu+2 and 1 at pH between 7 to 7.5. The stoichiometry binding ratio between chemosensor (1) and Cu+2 was determined by Job’s plot and it was found to be 1:2. The current study explored the use of these Schiff bases for the first time as heterocyclic chemosensors. DPPH radical scavenging, urease enzyme inhibition activities, molecular docking simulation, and density functional theory (DFT) analysis of compounds 1, 2, and 3 were also conducted.]]> <![CDATA[Synthesis and Molecular Docking Study of Some New Thiazole-coumarin Molecular Hybrids as Antibacterial Agents]]>https://www.benthamscience.com/article/1328052024-03-12Background: The emergence of drug-resistant bacteria and multidrug-resistant diseases, both of which are associated with high mortality, has posed a serious global health issue. Thiazoles and coumarins were reported as antimicrobial agents.

Objective: This research paper aims to describe the synthesis of some novel thiazole derivatives bearing a coumarin residue as antibacterial agents

Methods: The thiazole - coumarin hybrids were synthesized starting from the condensation of 3-acetyl coumarin (1) hydrazine carbothioamide (2) or thisemicarbazide then reacting the resulting products with different p-substituted phenacyl bromides (4a-e), hydrazonoyl chlorides (8a-e), and (11). In vitro antibacterial activity was studied in this work. In addition, molecular docking studies for the new compounds have also been carried out to investigate the binding mode of actions against the target DNA gyrase B.

Results: Some of the newly synthesized compounds such as compounds 10b, 7, and 6b showed pronounced activities against Gram (+ve) and Gram (-ve) bacteria compared to a reference antibacterial agent. Compounds 10b, 7, and 6b exhibited the best binding affinity against the target

Conclusion: We could obtain a series of precious hitherto unknown thiazole derivatives with varied antibacterial activities from cheap laboratory-available starting material following rather simple environmentally friendly techniques avoiding the use of hazardous or heavy metal-containing catalysts.

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