Synthesis and Pharmacological Evaluation of substituted (Benzothiazol-2-YL)-3-Phenylthiourea Derivatives

Abstract

A series of some novel (Benzothiazole-2-yl)-3-phenylthiourea Derivatives were synthesized and evaluated for anti-inflammatory activity. The titled compounds were synthesized from the substituted aromatic amines through the intermediate substituted 1-phenylthiourea oxidation by bromine water in acidic medium then reacted with Phenylisothiocyanate. The purity of the synthesized compounds were confirm by TLC and the structure was analyzed on the basis of IR and Mass spectral data. The anti-inflammatory activities of new compounds were determined by Carrageenan-induced rat paw edema method using diclofenac sodium as a standard. Among the compounds tested three compounds NP-x2(1-(6-methoxy-1,3-benzothiazol-2-yl)-3- phenylthiourea),NP-x3(1-(5-methoxy-1,3-benzothiazol-2-yl)-3 phenylthiourea),NP-x4(1-(6-methoxy-1,3-benzothiazol-2-yl)-3- phenylthiourea) were the most active compounds in these series when compared with diclofenac sodium. In the SAR study, Methyl and Methoxy groups substituted 1-(benzthiazol-2-yl)-3-phenylthiourea more antiinflammatory activity than halogen substituted 1-(benzthiazol-2-yl)-3- phenylthiourea derivative