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Synthesis, Pharmacological Evaluation And QSAR Studies Of 4,5-Dihydro-4-[(Substituted Phenyl) Methylene]-5-Oxo-2-Phenyl/Methyl-1H-Imidazole-1-Acetic Acids

Author(s): K Bharathi, K. V. S. R. G Prasad, M. N. A Rao

A series of (Z)-4,5-dihydro-4-[(substituted phenyl)methylene]-5-oxo-2-phenyl-1H-imidazole-1-acetic acids (1-11) and a few of (Z)-4,5-dihydro-4-[(substituted phenyl)methylene]-2-methyl-5-oxo-1H-imidazole-1- acetic acids (12-14) were synthesized and evaluated for antiinflammatory activity. Ten compounds showed significant antiinflammatory activity. Compound 2 exhibited activity comparable to phenylbutazone. It also showed significant antiarthritic activity and was less ulcerogenic than phenylbutazone. Five compounds exhibited significant analgesic activity. Several compounds showed good activity in scavenging the stable free radical DPPH. QSAR studies suggested that none of the physicochemical parameters studied showed good correlation to the antiinflammatory activity.


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