4.7 Article

Synthesis and antibacterial activity of some new thiadiaza/triazaphospholes, thiadiaza/triaza/tetrazaphosphinines and thiadiaza/tetrazaphosphepines containing 1,2,4-triazinone moiety

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 44, Issue 11, Pages 4539-4546

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2009.06.022

Keywords

Synthesis; Phosphorus heterocycles; 1,2,4-Triazinone; Antibacterial agents

Funding

  1. The Egyptian Ministry of Higher Education and Scientific Research

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Some new thiadiaza/triazaphospholes, thiadiaza/triaza/tetrazaphosphinines and thiadiaza/tetrazaphosphepines fused with 6-methyl-1,2,4-triazin-5-one moiety were synthesized via reactions of alpha,beta-bifunctional compounds derived from 4-amino-3-mercapto-6-methyl-1,2,4-triazin-5(4H)-one (1) with various phosphorus reagents. The in vitro antibacterial activities of the synthesized compounds were evaluated against some bacterial strains. Compounds 16 and 21 exhibited good inhibitory activities against most the tested organisms with MIC values in the range 6.25-12.5 mu g/mL and lower cytotoxicity in comparison with the reference drugs. (C) 2009 Elsevier Masson SAS. All rights reserved.

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