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基于杯[4]芳烃的 1,3,4-噁二唑和噻二唑衍生物:设计、合成与生物评价。

Calix[4]arene based 1,3,4-oxadiazole and thiadiazole derivatives: design, synthesis, and biological evaluation.

机构信息

Department of Chemistry, School of Sciences, Gujarat University, Navrangpura, Ahmedabad, 380009 Gujarat, India.

出版信息

Org Biomol Chem. 2012 Mar 7;10(9):1785-94. doi: 10.1039/c2ob06730g. Epub 2012 Jan 16.

DOI:10.1039/c2ob06730g
PMID:22246169
Abstract

In the present investigation, we describe some novel calixarene based heterocyclic compounds (5a-5i) in which 1,3,4-oxadiazole and 1,3,4-thiadiazole derivatives have been coupled with 5,11,17,23-tetra-tert-butyl-25,27-bis(chlorocarbonyl-methoxy)-26,28-dihydroxy calix[4]arene. All the newly synthesized calixarene based heterocyclic compounds have been characterized by elemental analysis and various spectroscopic methods like FTIR, (1)H NMR, (13)C NMR, and FAB-MS. All the final scaffolds have been subjected to antioxidant activity, in vitro antimicrobial screening against two gram (+ve) bacteria (S. aureus, S. pyogenes), two gram (-ve) bacteria (E. coli, P. aeruginosa) and two fungal strains (C. albicans, A. clavatus) and also have been screened for their antitubercular activity against Mycobacterium tuberculosis H(37)Rv.

摘要

在本研究中,我们描述了一些新型杯芳烃杂环化合物(5a-5i),其中 1,3,4-噁二唑和 1,3,4-噻二唑衍生物与 5,11,17,23-四叔丁基-25,27-双(氯甲酰基-甲氧基)-26,28-二羟基杯[4]芳烃偶联。所有新合成的杯芳烃杂环化合物均通过元素分析和各种光谱方法(如 FTIR、1H NMR、13C NMR 和 FAB-MS)进行了表征。所有最终支架都经过了抗氧化活性、体外抗两种革兰氏阳性(+ve)细菌(金黄色葡萄球菌、化脓性链球菌)、两种革兰氏阴性(-ve)细菌(大肠杆菌、铜绿假单胞菌)和两种真菌(白色念珠菌、棒状杆菌)的抗菌筛选,以及对结核分枝杆菌 H(37)Rv 的抗结核活性筛选。

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