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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and in vitro microbiological evaluation of novel 4-aryl-5-isopropoxycarbonyl-6-methyl-3,4-dihydropyrimidinones.
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Synthesis and in vitro microbiological evaluation of novel 4-aryl-5-isopropoxycarbonyl-6-methyl-3,4-dihydropyrimidinones.

机译：新型4-芳基-5-异丙氧基羰基-6-甲基-3,4-二氢嘧啶酮的合成及体外微生物学评价。

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摘要

Seven 4-aryl-5-isopropoxycarbonyl-6-methyl-3,4-dihydropyrimidin-2(1H)-ones 4a-g and 4-phenyl-5-isopropoxycarbonyl-6-methyl-3,4-dihydropyrimidin-2(1H)-thione 4h have been synthesized by a one-pot cyclocondensation of aldehydes, isopropyl acetoacetate and urea/thiourea in ethanol by using strontium chloride hexahydrate as the catalyst. All the compounds were screened for their antibacterial activity against Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa and Salmonella typhi and antifungal activity against Candida albicans, Aspergillus flavus, Rhizopus and Mucor. Compounds 4b, 4c, 4f, 4g exhibited excellent in vitro antibacterial activity against Staphylococcus aureus, Salmonella typhi and Pseudomonas aeruginosa and potent in vitro antifungal activity against Candida albicans, Rhizopus and Mucor. Compound 4f with a nitro group at the para position of the 4-aryl group and 4g with a fluorine at the para position of the 4-aryl group showed more activity than the standard drugs.
机译：七个4-芳基-5-异丙氧基羰基-6-甲基-3,4-二氢嘧啶-2（1H）-a 4g和4-苯基-5-异丙氧基羰基-6-甲基-3,4-二氢嘧啶-2（1H）用六水合氯化锶作催化剂，通过乙醇中的醛，乙酰乙酸异丙酯和尿素/硫脲的一锅环缩合反应合成了1）-硫酮4h。筛选所有化合物对金黄色葡萄球菌，大肠杆菌，肺炎克雷伯菌，铜绿假单胞菌和伤寒沙门氏菌的抗菌活性以及对白色念珠菌，黄曲霉，根霉和Mucor的抗真菌活性。化合物4b，4c，4f，4g对金黄色葡萄球菌，鼠伤寒沙门氏菌和铜绿假单胞菌具有出色的体外抗菌活性，并且对白色念珠菌，根霉和Mucor具有强大的体外抗菌活性。在4-芳基对位的硝基具有化合物的化合物4f和在4-芳基对位的氟具有4g的化合物显示出比标准药物更高的活性。

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