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

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

Volume: 9 Issue: 6

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

Affiliation:

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

Abstract: 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.

Cite this article as:

Plech Tomasz, Wujec Monika, Kosikowska Urszula, Malm Anna, Barylka Magdalena, Chalas Aleksandra and Kapron Barbara, The Effect of N-4 Substituent on Antibacterial Activity of Novel Hydroxymethyl/Aminomethyl Derivatives of 1,2,4-Triazole-3-thione, Letters in Drug Design & Discovery 2012; 9 (6) . https://dx.doi.org/10.2174/157018012800673056