ONE-POT THREE-COMPONENT MICROWAVE-ASSISTED SYNTHESIS OF NOVEL THIAZOLIDINONE DERIVATIVES CONTAINING THIENO[d]PYRIMIDINE-4-ONE MOIETY AS POTENTIAL ANTIMICROBIAL AGENTS.

Bioorganicheskaia khimiia Pub Date : 2015-05-01
I H El Azab, Sh H Abdel-Hafez
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Abstract

New 2-methyl-5-(4-oxo-2-(substituted phenyl)thiazolidin-3-yl)thieno[3,4-d]-pyrimidin-4-one, 5-(2,7-diphenyl-5-thioxo-5,6,7,7a-tetrahydrothiazolo[4,5-d]pyrimidin-3(2H)-yl)-2-methylthieno[3,4-d]pyrimidin-4(3H)-one, and 2-methyl-5-(5-phenyl-thiazolo[5,4-d]soxazol-6(5H)-yl)thieno[3,4-d]pyrimidin-4(3H)-one have been prepared under microwave-assisted and conventional conditions. The new compounds were screened for their in vitro antimicrobial activity against two gram-positive bacteria (Bacillus subtilis NCI M-2063 and Staphylococcus aureus NCIM-2901), one gram-negative bacteria (Escherichia coli NCIM-2256), and.three fungal strains (Candida albicans NCIM-3471, Aspergillusfiavus NCIM-539, and Aspergillus niger NCIM-1196) and showed promising biological activity.

一锅三组分微波辅助合成新型噻唑烷酮衍生物含噻诺嘧啶-4- 1片段作为潜在抗菌剂。
在微波辅助和常规条件下制备了新的2-甲基-5-(4-氧-2-(取代苯基)噻唑-3-基)噻吩[3,4-d]-嘧啶-4- 1,5-(2,7-二苯基-5-硫氧-5,6,7,7 -a -四氢噻唑[4,5-d]嘧啶-3(2H)-基)-2-甲基噻吩[3,4-d]嘧啶-4(3H)- 1和2-甲基-5-(5-苯基噻唑[5,4-d]索沙唑-6(5H)-基)噻吩[3,4-d]嘧啶-4(3H)- 1。新化合物对2种革兰氏阳性菌(枯草芽孢杆菌NCI M-2063和金黄色葡萄球菌NCI -2901)、1种革兰氏阴性菌(大肠杆菌NCI -2256)和1种革兰氏阴性菌的体外抑菌活性进行了筛选。3株真菌(白色念珠菌NCIM-3471、曲霉NCIM-539和黑曲霉NCIM-1196)显示出良好的生物活性。
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