Aboulwafa O M, Ismail K A, Koreish E A
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, Egypt.
Farmaco. 1992 May;47(5):631-42.
Two series of novel 3-carbethoxy-2-(3',4'-disubstituted-2',3'- dihydrothiazol-2'-ylidenamino)-4,5,6,7-tetrahydrobenzo[b] thiophenes (3a-o) and 2-methyl-3-(3',4'-disubstituted-2',3'-dihydrothiazol-2'-ylidena mino-5,6,7,8- tetrahydrobenzothieno[2,3-d]pyrimidin-4(3H) ones (8a-o) have been synthesized and tested for antimicrobial activity. All members of the series have been found to exhibit in vitro antibacterial and/or antifungal activities. Activity was optimized by cyclization to the thienopyrimidin-4-ones. In particular, compounds 8e and 8fd were the most active against the 3 tested microorganisms. Their antifungal activity was higher than that exhibited by nystatin while their MIC was found to be nearly equal to that of nystatin.
合成了两个系列的新型3-乙氧羰基-2-(3',4'-二取代-2',3'-二氢噻唑-2'-亚基氨基)-4,5,6,7-四氢苯并[b]噻吩(3a-o)和2-甲基-3-(3',4'-二取代-2',3'-二氢噻唑-2'-亚基氨基)-5,6,7,8-四氢苯并噻吩并[2,3-d]嘧啶-4(3H)酮(8a-o)，并对其抗菌活性进行了测试。已发现该系列的所有成员均表现出体外抗菌和/或抗真菌活性。通过环化生成噻吩并嘧啶-4-酮来优化活性。特别地，化合物8e和8fd对3种测试微生物的活性最高。它们的抗真菌活性高于制霉菌素，而其最低抑菌浓度与制霉菌素相近。
