Synthesis and antibacterial activity of some new thiadiaza/triazaphospholes, thiadiaza/triaza/tetrazaphosphinines and thiadiaza/tetrazaphosphepines containing 1,2,4-triazinone moiety.
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 microg/mL and lower cytotoxicity in comparison with the reference drugs.
Ali
Tarik El-Sayed
Tel-S
Department of Chemistry, Faculty of Education, Ain Shams University, Roxy, 11711 Cairo, Egypt.
D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001156:Artemia / Q000187:drug effects; D001419:Bacteria / Q000187:drug effects*; D001681:Biological Assay; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D017553:Phosphorus Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014227:Triazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
D000900:Anti-Bacterial Agents; D017553:Phosphorus Compounds; D014227:Triazines