Synthesis of new 2,5-Disubstituted-1,3,4-thiadiazoles and preliminary evaluation of anticonvulsant and antimicrobial activities

• Published in: Bioorganic & medicinal chemistry 2002-09, Vol.10 (9), p.2893-2898
• Main Authors: Dogan, Hatice N, Duran, Arzu, Rollas, Sevim, Sener, Göksel, Uysal, Meral K, Gülen, Dumrul
• Format: Article
• Language: English
• Subjects: Animals; Anti-Bacterial Agents - administration & dosage; Anti-Bacterial Agents - chemical synthesis; Anti-Bacterial Agents - pharmacology; Antibacterial agents; Antibiotics. Antiinfectious agents. Antiparasitic agents; Anticonvulsants - administration & dosage; Anticonvulsants - chemical synthesis; Anticonvulsants - pharmacology; Anticonvulsants. Antiepileptics. Antiparkinson agents; Biological and medical sciences; Drug Evaluation, Preclinical; Medical sciences; Mice; Mice, Inbred BALB C; Microbial Sensitivity Tests; Neuropharmacology; Pharmacology. Drug treatments; Pseudomonas aeruginosa - drug effects; Seizures - drug therapy; Thiadiazoles - administration & dosage; Thiadiazoles - chemical synthesis; Thiadiazoles - pharmacology
• ISSN: 0968-0896; 1464-3391
• DOI: 10.1016/S0968-0896(02)00143-8

Two new series of 2,5-disubstituted-1,3,4-thiadiazoles were synthesized for their possible anticonvulsant, antibacterial and antifungal activities. The degree of protection afforded by these compounds at a dose of 100 mg/kg ip against pentylenetetrazole-induced convulsions in mice ranged from 0 to 90%. Among these compounds, 2a (90%) and 2g (70%) showed maximum protection. Antimicrobial tests showed that the MIC value of 3j against Pseudomanas aeruginosa was equal to that of penicillin. 1,3,4-Thiadiazoles were synthesized. The degree of protection afforded by these compounds against PTZ-induced convulsions in mice ranged from 0 to 90%. Antimicrobal tests showed that the MIC value of 3j against Pseudomanas aeruginosa was equal to that of penicillin.