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一锅两步法简便合成2,3,4,5-四取代二氢恶唑及其抗菌活性

One-pot two-step facile synthesis of 2,3,4,5-tetra substituted dihydrooxazoles and their antimicrobial activity.

作者信息

Tiwari Shailendra, Pathak Poonam, Pratap Singh Kamal, Sagar Ram

机构信息

Department of Chemistry, University of Allahabad, Allahabad (UP) 211002, India.

Department of Chemistry, University of Allahabad, Allahabad (UP) 211002, India.

出版信息

Bioorg Med Chem Lett. 2017 Aug 15;27(16):3802-3805. doi: 10.1016/j.bmcl.2017.06.062. Epub 2017 Jun 24.

DOI:10.1016/j.bmcl.2017.06.062
PMID:28676271
Abstract

New 2,3,4,5-tetra substituted dihydrooxazoles derivatives were efficiently synthesized starting from benzaldehyde, aryl thiosemicarbazide and benzoin using designed synthetic route. Newly synthesized 2,3,4,5-tetra substituted dihydrooxazole derivatives were screened for their antibacterial and antifungal activities against different strains of pathogenic bacteria and fungi. The minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC) and minimum fungicidal concentration (MFC) were determined for the test compounds using positive and negative control. Compounds 4b, 4d, 4f, 4i, 4k and 4m, have shown good antibacterial activity whereas compounds 4e, 4g, 4h, 4j, 4l and 4n have displayed better antifungal activity.

摘要

从苯甲醛、芳基硫代氨基脲和安息香出发,通过设计的合成路线高效合成了新型2,3,4,5-四取代二氢恶唑衍生物。对新合成的2,3,4,5-四取代二氢恶唑衍生物针对不同病原菌和真菌菌株的抗菌和抗真菌活性进行了筛选。使用阳性和阴性对照测定了测试化合物的最低抑菌浓度(MIC)、最低杀菌浓度(MBC)和最低杀真菌浓度(MFC)。化合物4b、4d、4f、4i、4k和4m表现出良好的抗菌活性,而化合物4e、4g、4h、4j、4l和4n表现出较好的抗真菌活性。

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