Evaluation of antimycobacterial and anticonvulsant activities of new 1-(4-fluorobenzoyl)-4-substituted-thiosemicarbazide and 5-(4-fluorophenyl)-4-substituted-2,4-dihydro-3H-1,2,4-triazole-3-thione derivatives.
Some new 1-(4-fluorobenzoyl)-4-alkyl/arylthiosemicarbazide (2a-g), 5-(4-fluorophenyl)4-alkyl/aryl-2,4-dihydr-3H-1,2,4-triazole-3-thio ne (3a-g) derivatives, 3-(benzylthio)-5-(4-fluorophenyl)-4-phenyl-4H-1,2,4-triazole (3h) and 2-acetyl-5-(4-fluorophenyl)-4-phenyl-2,4-dihydro-3H-1,2,4-triazole-3-thi one (3i) were prepared and tested for their antimycobacterial and anticonvulsant activities. The structure of compounds was confirmed by elemental analyses and spectroscopic techniques. The antimycobacterial activity of the synthesized compounds was investigated against M. fortiutum ATCC 6841 and most of them were found active against the above strain with MIC values of 64 or 32 micrograms/ml. The anticonvulsant activity of the 2d, 3d-i was determined against pentylenetetrazole induced seizures. 3f-i showed anticonvulsant activity (10 to 30% protection).
Gülerman
N
N
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Marmara University, Istanbul, Turkey.
Rollas
S
S
Kiraz
M
M
Ekinci
A C
AC
Vidin
A
A
D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000927:Anticonvulsants / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D005069:Evaluation Studies as Topic; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D019907:Mycobacterium fortuitum / Q000187:drug effects*; D012663:Semicarbazides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
D000900:Anti-Bacterial Agents; D000927:Anticonvulsants; D012663:Semicarbazides; D014230:Triazoles