Synthesis and in vitro antimicrobial activity of new 4-phenyl-5-methyl-4H-1,2,4-triazole-3-thione derivatives.
This study presents the synthesis, spectral analysis and antimicrobial evaluation of a new series of substituted 1,2,4-triazole (5a-i) and 1,3,4-thiadiazole derivatives (9a, c, g, h). New compounds were obtained by cyclization reaction of acyl thiosemicarbazide derivatives in the presence of alkaline and acidic media. All synthesized compounds were screened for their in vitro antimicrobial activities. Nine of the compounds had potential activity against Gram-positive bacteria (MIC = 3.91-500 µg/mL). Some compounds showed good activity especially against: Micrococcus luteus ATCC 10240 (MIC = 3.91-31.25 µg/mL), Bacillus subtilis ATCC 6633 (MIC = 15.63- 62.5 µg/mL), and Staphylococcus aureus ATCC 25923 (MIC = 15.63-125 µg/mL).
Department of Organic Chemistry, Medical University, Lublin, Poland. lukasz.popiolek@umlub.pl
Łukasz
Ł
Popiołek
Urszula
U
Kosikowska
Maria
M
Dobosz
Anna
A
Malm
D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D060326:Chemistry Techniques, Synthetic; D003500:Cyclization; D004353:Drug Evaluation, Preclinical / Q000379:methods; D006094:Gram-Positive Bacteria / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D016982:Micrococcus luteus / Q000187:drug effects; D013211:Staphylococcus aureus / Q000187:drug effects; D013830:Thiadiazoles / Q000737:chemistry; D014230:Triazoles / Q000737:chemistry
D000890:Anti-Infective Agents; D013830:Thiadiazoles; D014230:Triazoles; C058949:1,3,4-thiadiazole; C045575:1,2,4-triazole