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Arch Pharm Res ; 27(9): 885-92, 2004 Sep.
Article in English | MEDLINE | ID: mdl-15473655

ABSTRACT

Due to the rapidly growing number of resistant strains of bacteria, the search for antibacterial agents with new modes of action will always remain an important and challenging task. Thus, the reaction of 2-substituted or unsubstituted-4-(4-acetylanilino)-5,6,7,8-tetrahydrobenzo[b]thieno[2,3-d]pyrimidine derivatives 1-3 with the hydrazine derivatives, semi and/or thiosemicarbazides, provided the corresponding hydrazones 4-6 and semi and/or thiosemicarbazones 7-9. Claisen-Schmidt condensation of compounds 1 or 2 with the appropriate aldehyde yielded the chalcones 10, 11 which, when treated with hydroxylamine hydrochloride gave rise to the isoxazoline-containing compounds 12, 13. Furthermore, reacting the respective chalcones 10, 11 with different hydrazines, urea and/or thiourea, furnished compounds 14, 15, 16, and 17 respectively. Representative compounds were tested for their antimicrobial activity against Candida albicans and certain gram-positive and gram-negative bacteria. Their MICs were then determined. Compound 15e, showed a broad spectrum of activity while most of the other compounds showed varying antimicrobial activity.


Subject(s)
Anti-Bacterial Agents/chemical synthesis , Antifungal Agents/chemical synthesis , Pyrimidines/chemical synthesis , Anti-Bacterial Agents/pharmacology , Antifungal Agents/pharmacology , Candida albicans/drug effects , Candida albicans/growth & development , Microbial Sensitivity Tests/statistics & numerical data , Pyrimidines/pharmacology , Staphylococcus aureus/drug effects , Staphylococcus aureus/growth & development
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