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Synthesis and Antibacterial and Antifungal Activity of New Thieno[2,3-d]Pyrimidin-4(3H)-One Derivatives
Pharmaceutical Chemistry Journal ( IF 0.8 ) Pub Date : 2020-09-01 , DOI: 10.1007/s11094-020-02252-5
B. Kahveci , İ. S. Doğan , E. Menteşe , H. E. Sellitepe , D. Kart

A series of new 2-(4/3-substitutedbenzyl)thieno[2,3-d]pyrimidin-4(3H)-ones (2a-f) and 2-(4/3-substituted benzyl)-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one derivatives (3a-f) were synthesized for the first time by the reaction of corresponding 2-aminothiophene-3-carboxamide derivatives and appropriate iminoester hydrochlorides under suitable conditions. Using microdilution method, the antibacterial and antifungal activities of the synthesized compounds were tested against selected strains of Gram positive and Gram negative bacteria (Staphylococcus aureus, Enterecoccus faecalis, Escherichia coli and Pseudomonas aeruginosa) and yeast-like fungi (Candida albicans, C. krusei and C. parapsilosis). In these tests, compounds 3a-f showed higher antifungal activity than fluconazole against Candida fungus species. 2-Substituted thieno-[2,3-d]pyrimidin-4(3H)-ones (2a-f) showed better antibacterial activity than 2-substituted 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one derivatives (3a-f).

中文翻译:

新型噻吩并[2,3-d]嘧啶-4(3H)-One衍生物的合成及抗菌抗真菌活性

一系列新的2-(4/3-取代苄基)噻吩并[2,3-d]嘧啶-4(3H)-酮(2a-f)和2-(4/3-取代苄基)-5,6,通过相应的2-氨基噻吩-3-甲酰胺反应,首次合成了7,8-四氢苯并[4,5]噻吩并[2,3-d]嘧啶-4(3H)-酮衍生物(3a-f)衍生物和适当的亚氨基酯盐酸盐在合适的条件下。使用微量稀释方法,对选定的革兰氏阳性菌和革兰氏阴性菌(金黄色葡萄球菌、粪肠球菌、大肠杆菌和铜绿假单胞菌)和酵母样真菌(白色念珠菌、克柔念珠菌)测试合成化合物的抗菌和抗真菌活性和 C. 近平滑肌)。在这些测试中,化合物 3a-f 显示出比氟康唑更高的抗念珠菌活性。2-取代的噻吩-[2,
更新日期:2020-09-01
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