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Letters in Drug Design & Discovery


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

The Effect of N-4 Substituent on Antibacterial Activity of Novel Hydroxymethyl/Aminomethyl Derivatives of 1,2,4-Triazole-3-thione

Author(s): Tomasz Plech, Monika Wujec, Urszula Kosikowska, Anna Malm, Magdalena Barylka, Aleksandra Chalas and Barbara Kapron

Volume 9, Issue 6, 2012

Page: [633 - 637] Pages: 5

DOI: 10.2174/157018012800673056

Price: $65


Several new, N2-substituted derivatives of 1,2,4-triazole-3-thione were synthesised in order to analyse the impact of substituent in the N-4 position on antibacterial activity. Structure of the compounds in question was confirmed on the basis of 1H NMR and IR spectra as well as by means of the elementary analysis (C, H, N). Microbiological studies were conducted on Gram-positive and Gram-negative bacteria strains. One of the compounds inhibited growth of Bacillus cereus ATCC 10876 with the same efficiency as ampicillin. The analysis of the structure-activity relationship indicated that introduction of a chlorine atom into the phenyl ring in the N-4 position significantly improved antibacterial activity.

Keywords: Aminomethylation, Hydroxymethylation, Mannich bases, MRSA, Opportunistic bacteria, SAR

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