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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和体外微生物评价。

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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：7-芳基-5-异丙氧基羰基-6-甲基-3,4-二氢嘧啶-2（1H） - 酮4a-g和4-苯基-5-异丙氧基羰基-6-甲基-3,4-二氢嘧啶-2（1h ） - 通过使用氯化锶六水合物作为催化剂，通过使用氯化锶，异丙基乙酸乙酯和尿素/硫脲脲/硫脲的单罐环核缩聚合成4H。筛选所有化合物对其对葡萄球菌，大肠杆菌，Klebsiella肺炎，假单胞菌铜绿素和沙门氏菌的抗菌活性进行抗菌活性，对念珠菌蛋白质，曲霉素，根瘤菌和粘膜抗真菌活性。化合物4b，4c，4f，4g对葡萄球菌，沙门氏菌和假单胞菌铜绿假单胞菌以及针对念珠菌和粘膜的有效的体外抗真菌活性表现出优异的体外抗菌活性。在4-芳基的对位位置和4-芳基的PARA位置的4-芳基的PARA位置的化合物4f与4-芳基的氟，表现出比标准药物更多的活性。

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