SYNTHESIS, IN VITRO ANTI INFLAMMATORY ACTIVITY AND QSAR EVALUATION OF BENZOTRIAZOLYL-3-(2-HYDROXYPHENYL) PROP-2-ENOIC ACID DERIVATIVES

C. M. Jamkhandi*, J. I. Disouza, S. D. Asgekar, T. B. Sutar, P. S. Kumbhar

ABSTRACT

The objective of the present work is to synthesize novel (2E)-2-(1H-benzotriazol-1-yl)-3-{2-hydroxy-5-[(E)-phenyldiazenyl]phenyl}prop-2-enoic acid derivatives. The synthesis of derivatives is based on daizonium coupling reactions. The intermediate compound (2E)-2-(1H-benzotriazol-1-yl)-3-(2-hydroxyphenyl)prop-2-enoic acid was subjected to diazonium coupling reaction with aromatic amines resulting in formation Benzotriazole substituted propenoic acid derivatives (Id to VId). The structure of the synthesized derivatives was confirmed with Physical constants, TLC, IR NMR and Mass spectroscopy. Then derivatives were screened for in vitro anti inflammatory activity using egg albumin method. QSAR Evaluation of the compounds was done using dependent and independent variables based Hansch approach.

Keywords: Benzotriazole, Diazonium Coupling Reaction, Aromatic amines, QSAR evaluation.