Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


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, Barbara Kapron.


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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Article Details

Year: 2012
Page: [633 - 637]
Pages: 5
DOI: 10.2174/157018012800673056
Price: $58