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Synthesis of some new pyrimidine-azitidinone analogues and their antioxidant, in vitro antimicrobial, and antitubercular activities

机译：某些新型嘧啶-氮杂环丁酮类似物的合成及其抗氧化剂，体外抗菌剂和抗结核活性

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A series of 1-(3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)-4-methylphenyl)-3-chloro-4-(2-mercaptoquinolin-3-yl)azetidin-2-one (7a-j) have been synthesized from the condensation of aromatic amines with N-phenylacetamide. The thione nucleus formed from 2-chloroquionoline-3-carbadehyde using sodium sulphide in dimethyl formamide (DMF) was followed by the reaction with pyrimidine amine to form the Schiff base intermediates. Attempt has been made to derive final azetidinone analogues from Schiff bases by using chloroacetyl chloride. The newly synthesized analogues were examined for the antimicrobial activity against some bacterial and fungal strains and in vitro antituberculosis activity against mycobacterium tuberculosis. These observations provide some predictions to design further antibacterial and antituberculosis active compounds prior to their synthesis according to molecular studies.

机译：一系列的1-（3-（4-（吡啶-3-基）嘧啶-2-基氨基）-4-甲基苯基）-3-氯-4-（2-巯基喹啉-3-基）氮杂环丁烷-2-一（7a-j）是由芳族胺与N-苯基乙酰胺的缩合反应合成的。使用二甲基甲酰胺（DMF）中的硫化钠，由2-氯喹啉-3-碳氢化物形成的硫酮核，然后与嘧啶胺反应形成席夫碱中间体。已经尝试通过使用氯乙酰氯从席夫碱衍生出最终的氮杂环丁酮类似物。检查了新合成的类似物对某些细菌和真菌菌株的抗微生物活性以及对结核分枝杆菌的体外抗结核活性。这些观察结果提供了一些预测，以便根据分子研究在合成之前进一步设计抗菌和抗结核活性化合物。

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Chandrashekaraiah M.; Lingappa M.; Vathsala D. C.; Bhadregowda D. G.;
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年度 2014
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机译：腙类似物：分子建模，合成，体内抗伤害活性和体外抗微生物活性

Synthesis of some new pyrimidine-azitidinone analogues and their antioxidant, in vitro antimicrobial, and antitubercular activities

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