Preparation and antibacterial activity of 3-methyl-1-p-substituted phenylpyrazole-5-thiol.
3-Methyl-1-phenylpyrazole-5-thiol (3a) and its p-nitro- (5) and p-fluorophenyl (8) derivatives were prepared as potential antimicrobial agents in relatively good yields. Compounds 3a and 8 showed good antibacterial activities against MRSA, S. aureus, S. epidermidis, E. faecalis, E. faecium, and S. pyogenes. Moreover, compound 3a also showed a synergistic effect with some aminoglycosides.
Tagawa
Yoshinobu
Y
Faculty of Pharmaceutical Sciences, Fukuoka University, 8-19-1 Nanakuma, Jonan-ku, Fukuoka 814-0180, Japan. tagawa@fukuoka-u.ac.jp
Minami
Shin'ichi
S
Yoshida
Toshio
T
Tanaka
Keitaro
K
Sato
Shuji
S
Goto
Yoshinobu
Y
Yamagata
Kenji
K
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D006094:Gram-Positive Bacteria / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013438:Sulfhydryl Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*
C457901:3-methyl-1-(p-fluorophenyl)pyrazole-5-thiol; C457900:3-methyl-1-(p-nitrophenyl)pyrazole-5-thiol; C457899:3-methyl-1-phenylpyrazole-5-thiol; D000900:Anti-Bacterial Agents; D011720:Pyrazoles; D013438:Sulfhydryl Compounds