Recent Advancement and Structure Activity Paradigm of Benzothiazoles: A Classical Review for Biological Screening of Different Diseases

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Authors: Md Afaque, Abdullah*, Md Sabir Hussain Siddiquee, Md Shamsir Alam, Md Quamar Niyaz, Md Saddam Hussain, Md Iftekhar Alam
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Abstract

Heterocyclic compounds and their analogues have been extensively studied for their diverse pharmacological properties, including antimicrobial, anti-malarial, anti-inflammatory, anti-tubercular, anti-diabetic, and anti-neoplastic activities. The benzothiazole nucleus, despite its simple and compact structure, serves as a privileged scaffold in medicinal chemistry, demonstrating a remarkable spectrum of biological activities. This review consolidates recent advancements in the chemistry of benzothiazoles, focusing on the synthesis, structural modifications, and the resultant Structure-Activity Relationship (SAR) that underpin their biological efficacy. Significant structural modifications have revealed the potent activity of benzothiazole derivatives against various microbial strains and cancer cell lines. This summary primarily focuses on the benzothiazole core and its substituted analogues, elucidating their diverse biological profiles and potential as leads for future therapeutic agents.

Fields of Study & Subjects

Synthesis and biological activity Synthesis and Characterization of Heterocyclic Compounds Phenothiazines and Benzothiazines Synthesis and Activities

Publication details

Journal / source
Zenodo (CERN European Organization for Nuclear Research)
Publication date
9 February 2026