Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry and Computational Chemistry


Synthesis and Screening of New Isatin Derivatives

Author(s): B.Srinivas, V.Rajini Priya, G.Sridhar Babu, J.Venkateshwar Rao, P.S. Malathy, K.Raja Manohar, B.Chandara Prakash, L.Srikanth

In view of the biological prominence of isatin derivatives and benzimidazole derivatives, it is planned to synthesize new isatin derivatives containing 1-H-benzimidazol-2yl methane-thiol moiety in one side chain at 3rd position. So, some new 2-[1H-benzimidazol-2-ylmethyl) sulfanyl]-N'-[(3Z)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]aceto hydrazides (VIII) have been synthesized as depicted in scheme-I. The intermediates and final compounds were purified and their chemical structures have been confirmed by IR, 1H NMR, Mass and by elemental analysis. Investigation of anti-inflammatory activity was done by carrageenan induced rat hind paw edema method. Among the compounds tested, Compounds (VIIIc) & (VIIId) with methyl group at 5th and 7th positions of the indole ring exhibited maximum activity with percentage inhibition of 68.56 and 61.41. Compounds VIIIi(R=5-COOH), VIIIg(R=5-Cl), VIIIh(R=7-Cl), VIIIb(R=5-Br), VIIIf(R=7-NO2), VIIIe(R=5-NO2) and VIIIa(R=H) were found to be next in the order of antiinflammatory activity.

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