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ISSN 2063-5346
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DESIGN, SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF NOVEL 2-(1-BENZYL-2-OXOINDOLIN-3-YLIDENE)-N-PHENYLHYDRAZINECARBOXAMIDE DERIVATIVES.

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Araka sushma1*, Dr. Shivaraj2
» doi: 10.48047/ecb/2023.12.si10.00301

Abstract

Novel 2-(1-benzyl-2-oxoindolin-6-substituted-3-ylidene)-n-phenyl hydrazine carboxamide derivatives are an important class of nitrogen containing heterocyclic’s and were identified as the most active and potent classes of compounds with wide range of biological and pharmacological activities. A new series of 2-(1-benzyl-2-oxoindolin-3-ylidene)-n-phenyl hydrazine carboxamide derivatives were characterized by spectral data and evaluated for Anticancer activity, Anti-Alzheimer’s activity and anti-microbial activity. The compounds 7d, 7i, were found to be good inhibitors of HELa and MCF-7. Most of the compounds inhibited HELa and MCF-7with the IC50 values, ranging from 0.78μM 7.64 μM. Amongst them, compounds 7d, 7i with fluoro substituted indole exhibited strongest inhibitory activity against HELa and MCF-7 with IC501.91±0.02 μM, 0.92±0.03 μM for 7d and 7i 1.31±0.02μM, 0.78±0.3 respectively, when compared to standard Cisplain with IC50 of 0.65±0.02 μM and 0.47±0.02. The compound 7i with fluoro substituted indole containing Schiff base showed potent anti-Alzheimer’s activity with IC50 values 0.92±0.13, 1.01±0.12μM against AChE and BuChE respectively when compared to Standard drug donepazil showed IC50 0.51±0.06 and 0.31±0.04μM against AChE and BuChE respectively. 7i ,7m & 7n showing potent activity for different strains of bacteria ranging from 10mm to 14mm when compared to ciprofloxacin 13- 16mm. Thus, these Novel 2-(1-benzyl-2-oxoindolin-3-ylidene)-n-phenyl hydrazine carboxamide derivatives have emerged as new cancer, AChE and BuChE inhibitors and showing anti microbial activity for further exploitation as anti-cancer and anti-Alzheimer’s agents, anti bacterial agents. Docking studies of all the molecules disclosed close hydrogen bond interactions with in the binding site.

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