In-Silico and In-Vitro Approaches to Screen the Antituberculosis Activity of Benzothiazole Analogs

Introduction to Benzothiazole as a Drug Moiety

Author(s): Mahesh Bhat, S.L. Belagali, B. Manohara and B.K. Sagar

Pp: 1-18 (18)

DOI: 10.2174/9789811494635121010004

* (Excluding Mailing and Handling)


Benzothiazole (1, 3-benzothiazole) is one of the important fused heterocyclic compounds, which is a weak base having varied biological activities. The unique methyne center present in the thiazole ring makes benzothiazole as the most bioactive heterocyclic compound. The benzothiazole subunit is the commonly found in many natural bioactive compounds and semisynthetic drugs. Benzothiazole and its analogous found to exhibit variety of bio-activities, also with less toxic effect and their derivatives showed the enhanced activities, which has proven Benzothiazole scaffold is one of the prominant moiety in the medicinal chemistry, presence of hetero atoms such as sulphur and nitrogen makes the receptor cite in the parent moiety for the observed activity. Benzothiazole derivatives possess various pharmacological activities such as anti-viral, anti-microbial, anti-allergic, anti-diabetic, anti-tumor, anti-inflammatory, anthelmitic and anti-cancer activities. Which makes chemistry of benzothiazole is makes the prominent, rapidly developing and interesting field in the medicinal chemistry. In this chapter, briefly explained the importance, common methods of synthesis of the benzothiazole scaffold and also explained the popular benzothiazole molecules which have applications in various fields of the chemistry. Main objective of this chapter to explore various pharmacological activities containing benzothiazole moieties and rationalized the activities based on the structural variations with respect to the tuberculosis activity. The studies on benzothiazole derivatives reveal that, substitution on the C-2 and C-6 positions are the reasons for variety of biological activities.

Keywords: Activity, Benzothiazole, Cyclization, Docking, Docking score, DprE1, Guanidinyl, H37Rv Strain, Heterocycle, IC50, InhA, Luciferin, MIC, MTT, Pyrazole, SAR, TB activity, Thiazole, Triazole, Tuberculosis.

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