European Journal of Biomedical and Pharmaceutical Sciences

SYNTHESIS AND EVALUATION OFANTI-TUBERCULAR ACTIVITY OF BENZOTHIAZOLE DERIVATIVES

Gaware Vinayak Madhukar*, Dhamak Kiran Bhausaheb, Kotade Kiran Babasaheb

ABSTRACT

Derivatives of benzothiazoles were synthesized and evaluated for their anti-tubercular activity. 2-amino benzothiazole was first converted to 6 substituted derivatives of 2-amino benzothiazole by nitration and bromination reaction to yield 6-nitro-2-amino benzothiazole and 6-bromo-2-amino benzothiazole respectively. All the derivatives including 2-amino benzothiazole were further treated with chloroacetyl chloride to form chloroacetamido derivatives of benzothiazole. Further the product is treated with various heterocyclic and aromatic amines. The synthesized compounds were confirmed by IR, 1H NMR and Mass spectral data. Synthesized substituted benzothiazole derivatives were investigated for their anti-tubercular activity using Middle brook 7H9 agar medium as described by Elmer WK et al. against H37Rv Strain. It was observed that the new synthesized compounds possessing electron withdrawing group like nitro and bromo groups at 6th position of benzothiazole nucleus and chloro, fluoro substituted at 3rd position of aromatic amine exhibited higher anti-tubercular when compared to that of other synthesized compounds. The present research focus on the different methods of synthesis of substituted benzothiazoles with potential anti-tubercular activity that are now in developing phase.

Keywords: Anti-tubercular, Benzothiazole; Bromination; Chloroacetyl chloride; Nitration.