SYNTHESIS AND EVALUATION OF BENZOTHIAZOLE DERIVATIVES FOR ANTHELMINTIC ACTIVITY

Gaware Vinayak M.*, Dhamak Kiran B. and Kotade Kiran B.

ABSTRACT

Derivatives of benzothiazoles were synthesized and evaluated for their anthelmintic 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 anthelmintic activity against Indian adult earthworms (pheretima posthuma) at various concentrations (25 mg/ml and 50 mg/ml) .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 anthelmintic activity when compared to that of other synthesized compounds. The present research focus on the different methods of synthesis of substituted benzothiazoles with potential anthelmintic activity that are now in developing phase.

Keywords: Anthelmintic, Albendazole, Benzothiazole; Bromination; Nitration.