合成及一些新的噻吩[2,3-b]噻吩衍生物的抗菌活性。
Synthesis and antimicrobial activity of some new thieno[2,3-b]thiophene derivatives.
机构信息
Department of Chemistry, Faculty of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.
出版信息
Molecules. 2013 Apr 19;18(4):4669-78. doi: 10.3390/molecules18044669.
A series of thieno[2,3-b]thiophene moiety-containing bis-cyanopyrazoles 5a-c, bis-aminopyrazole 9 and bis-pyridazine derivatives 11 were synthesized and evaluated in vitro for their antimicrobial potential. The antimicrobial activity of some selected products was evaluated and showed good results. 5,5'-(3,4-Dimethylthieno[2,3-b]thiophene-2,5-diyl)bis(3-acetyl-1-(4-chlorophenyl)-1H-pyrazole-4-carbonitrile) (5d) was found to be more potent than the standard drug amphotericin B against Geotricum candidum and equipotent to amphotericin B against Syncephalastrum racemosum. In addition, it was found to be equipotent to the standard drug Penicillin G against Staphylococcus aureus. Moreover, it was more potent than the standard drug streptomycin against Pseudomonas aeruginosa and Escherichia coli.
一系列含有噻吩并[2,3-b]噻吩部分的双氰基吡唑 5a-c、双氨基吡唑 9 和双哒嗪衍生物 11 被合成并在体外评估其抗菌潜力。一些选定产物的抗菌活性进行了评估，结果良好。5,5'-(3,4-二甲基噻吩并[2,3-b]噻吩-2,5-二基)双(3-乙酰基-1-(4-氯苯基)-1H-吡唑-4-甲腈)（5d）对申克氏孢子丝菌的活性比标准药物两性霉素 B 更强，与两性霉素 B 对 Syncephalastrum racemosum 的活性相当。此外，它对金黄色葡萄球菌的活性与标准药物青霉素 G 相当。此外，它对铜绿假单胞菌和大肠杆菌的活性比标准药物链霉素更强。
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