Condensed bridgehead nitrogen heterocyclic system: synthesis and pharmacological activities of 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole derivatives of ibuprofen and biphenyl-4-yloxy acetic acid.
Several 3,6-disubstituted-1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazoles were prepared by condensation of 4-amino-5-substituted-3-mercapto-(4H)-1,2,4-triazoles (3a,b) with various substituted aromatic acids and aryl/alkyl isothiocyanates through a one-pot reaction. These compounds were investigated for their anti-inflammatory, analgesic, ulcerogenic, lipid peroxidation, antibacterial and antifungal activities. Some of the synthesized compounds showed potent anti-inflammatory activity along with minimal ulcerogenic effect and lipid peroxidation, compared to those of ibuprofen and flurbiprofen. Some of the tested compounds also showed moderate antimicrobial activity against tested bacterial and fungal strains.
Amir
Mohd
M
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hamdard University, New Delhi 110 062, India. mamir_s2003@yahoo.co.in
Kumar
Harish
H
Javed
S A
SA
D000208:Acute Disease; D000700:Analgesics / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use / Q000633:toxicity; D000818:Animals; D001419:Bacteria / Q000187:drug effects; D004158:Diphenylacetic Acids / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity; D005260:Female; D005658:Fungi / Q000187:drug effects; D022781:Hepatocytes / Q000187:drug effects; D007052:Ibuprofen / Q000031:analogs & derivatives* / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity; D007249:Inflammation / Q000188:drug therapy; D015227:Lipid Peroxidation / Q000187:drug effects; D008297:Male; D051379:Mice; D051381:Rats; D013830:Thiadiazoles / Q000737:chemistry*; D014230:Triazoles / Q000737:chemistry*; D014456:Ulcer / Q000209:etiology
D000700:Analgesics; D004158:Diphenylacetic Acids; D013830:Thiadiazoles; D014230:Triazoles; C045575:1,2,4-triazole; C037760:diphenylacetic acid; D007052:Ibuprofen