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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Synthesis and Biological Evaluation of Piperazinyl-2-(Benzo)thiophen/- furan-2-yl-acetonitriles as Strecker Reaction Products

Author(s): Rahul V. Patel, Jigar K. Patel, Shivraj H. Nile and Se Won Park

Volume 10, Issue 5, 2013

Page: [462 - 470] Pages: 9

DOI: 10.2174/1570180811310050014

Price: $65

Abstract

Single step construction of heterocyclic α-aminonitriles has been carried out using Indium Powder as catalyst in water medium via Strecker reaction methodology. The multicomponent reaction products were examined for their inhibitory potential against two Gram-positive bacteria (S. aureus and B. cereus), three Gram-negative bacteria (E. coli, P. aeruginosa and K. pneumoniae) and two fungal species (A. niger and C. albicans). The biological screening identified that the some compounds were found to possess promising antimicrobial (6.25-50 μg/mL of MIC) potential. A structure– activity relationship (SAR) study was explored to facilitate further development of this new class of compounds. The structural assignments of the new products were done on the basis of IR, 1H NMR, 13C NMR spectroscopy and elemental analysis.

Keywords: Thiophehe, Furan, piperazine, Indium powder, Catalyst, Antimicrobial activity


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