SYNTHESIS OF SOME N-ARYLAZOLE ACETAMIDE DERIVATIVES AND THEIR ANTICONVULSANT AND ANTIMICROBIAL ACTIVITIES


OZKANLI F. , DALKARA S. , CALIS U., WILLKE A.

ARZNEIMITTEL-FORSCHUNG/DRUG RESEARCH, ss.920-924, 1994 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Basım Tarihi: 1994
  • Dergi Adı: ARZNEIMITTEL-FORSCHUNG/DRUG RESEARCH
  • Sayfa Sayıları: ss.920-924

Özet

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, H-1-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 detemined 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 < 32 mu g/ml) against various Candida species.