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Med Chem Res. 2013 May;22(5):2531-2537. Epub 2012 Sep 29.

Microbiologically active Mannich bases derived from 1,2,4-triazoles. The effect of C-5 substituent on antibacterial activity.

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1
Department of Organic Chemistry, Faculty of Pharmacy, Medical University, Chodzki 4A, 20-093 Lublin, Poland.

Abstract

Our research proved that chemical character of the C-5 substituent significantly determines the antibacterial activity of the Mannich bases derived from 4,5-disubstituted 1,2,4-triazole-3-thiones. This activity was considerably increased by an introduction of a chlorine atom to the phenyl ring. The obtained compounds were particularly active against opportunistic bacteria (Bacillus subtilis and Bacilluscereus). The antibacterial activity of some Mannich bases was similar or higher than the activity of commonly used antibiotics such as ampicillin and cefuroxime.

KEYWORDS:

Aminomethylation; Five-membered ring; MRSA; Opportunistic bacteria

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