Synthesis of some N-arylazole acetamide derivatives and their anticonvulsant and antimicrobial activities
Ozkanli, F.; Dalkara, S.; Caliş, U.; Willke, A.
Arzneimittel-Forschung 44(8): 920-924
1994
ISSN/ISBN: 0004-4172 PMID: 7945533 Document Number: 433857
Some new N-arylazole acetamide derivatives have been prepared by the reaction of alpha-bromo-N-arylacetamide with imidazole, pyrazole and 1,2,4-triazole. The structures of these compounds have been confirmed by UV, IR, 1H-NMR and elementary analysis. Their anticonvulsant activities were determined by maximal electroshock (MES) and subcutaneous metrazol (Scmet) tests. Most of the compounds showed anticonvulsant activity with significantly low neurotoxicity according to Phase I tests. Compound 6 carrying alpha-naphthyl and 1,2,4-triazole was found active in the MES test with ED-50 = 64.9 mg/kg and TD-50 = 221.0 mg/kg but it was not active in corneally stimulated rats. Antibacterial and antifungal activities of the compounds were determined against S. aureus, E. coli, P. aeruginosa, C. albicans, C. parapsilosis, C. pseudotropicalis and C. stellatoidea by using the microdilution broth method Compounds 8 and 10 showed significant activity (MIC lt 32 mu-g/ml) against various Candida species.