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.
