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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis, antimicrobial activity, pharmacophore analysis of some new 2-(substitutedphenyl/benzyl)-5-((2-benzofuryl)carboxamido)benzoxazoles.
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Synthesis, antimicrobial activity, pharmacophore analysis of some new 2-(substitutedphenyl/benzyl)-5-((2-benzofuryl)carboxamido)benzoxazoles.

机译：一些新的2-（取代的苯基/苄基）-5-（（2-苯并呋喃基）羧酰胺基）苯并恶唑的合成，抗菌活性和药效团分析。

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摘要

The synthesis and antimicrobial activity of a new series of 2-(substitutedphenyl/benzyl)-5-[(2-benzofuryl)carboxamido]benzoxazole derivatives 3-12 were described. The in vitro antimicrobial activity of the compounds was determined against some Gram-positive, Gram-negative bacteria and fungi and their drug-resistant isolates in comparison with standard drugs. Antimicrobial results indicated that the synthesized compounds possessed a broad spectrum of activity with MIC values 500-15.625mug/ml. In the series, the most active compound against Candida krusei and Candida albicans isolate is 8 with MIC value 31.25mug/ml. However, it is one dilution less potent than the compared fluconazole. Some of the screened compounds exhibit significant activity, having MIC value as 31.25mug/ml in Pseudomonas aeruginosa having same activity as Rifampicin. Furthermore, considering the worth of developing new antibacterial agents against drug-resistant P. aeruginosa the present study explores the structure-activity relationship analysis of 2-(substitutedphenyl/benzyl)-5-[(2-benzofuryl)carboxamido]benzoxazoles using 3D-common features pharmacophore hypotheses approach.
机译：描述了一系列新的2-（取代的苯基/苄基）-5-[（2-苯并呋喃基）羧酰胺基]苯并恶唑衍生物3-12的合成和抗菌活性。与标准药物相比，确定了该化合物对某些革兰氏阳性，革兰氏阴性细菌和真菌及其耐药分离株的体外抗菌活性。抗菌结果表明合成的化合物具有广谱的活性，MIC值为500-15.625mug / ml。在该系列中，对克鲁斯假丝酵母和白色念珠菌分离物最有活性的化合物是8，MIC值为31.25mug / ml。但是，它的稀释度比氟康唑的稀释度低。某些被筛选的化合物显示出显着的活性，在铜绿假单胞菌中具有与利福平相同活性的MIC值为31.25mug / ml。此外，考虑到开发抗药性铜绿假单胞菌的新型抗菌剂的价值，本研究探索了使用3D-对2-（取代的苯基/苄基）-5-[（2-苯并呋喃基）甲酰胺基]苯并恶唑的构效关系分析药效团假设方法的共同特征。

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