Synthesis and biological screening of novel 2-morpholinoquinoline nucleus clubbed with 1,2,4-oxadiazole motifs
Synthesis and biological screening of novel 2-morpholinoquinoline nucleus clubbed with 1,2,4-oxadiazole motifs
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DOI：
10.1016/j.ejmech.2016.12.016
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发表时间：
2017-01-27
影响因子：
6.7
通讯作者：
Raval, Dipak K.
中科院分区：
文献类型：
--
作者：
Karad, Sharad C.;Purohit, Vishal B.;Raval, Dipak K.
设计并合成了一系列含1，2，4-恶二唑结构的新型2-吗啉代喹啉骨架（6a-n），产率为76-86%。筛选合成的化合物的初步体外抗微生物活性对一组致病菌株的细菌和真菌。对所合成的化合物进行了分子对接和药动学研究。采用S.粟酒裂殖酵母细胞在细胞水平。合成的化合物对S.在琼脂糖凝胶上观察到粟酒酵母。化合物6d、6 e、6 g、6 h、6 j和6 n与标准药物（即氨苄青霉素、诺氟沙星、氯霉素、环丙沙星）相比表现出优异的抗微生物效力。化合物6d、6 e、6 g、6 k和6 n与灰黄霉素相比具有显著的抗真菌活性。发现化合物6 f、6 i、6 k、61的细胞毒性非常小，而发现化合物6d、6 e、6 g、6 h表现出最大毒性。其余的合成化合物被发现具有中等毒性。(C)2016年由Elsevier Masson SAS出版。
Novel series of 2-morpholinoquinoline scaffolds (6a-n), containing the 1,2,4-oxadiazole and moiety, was designed and synthesized in good yield (76-86%). The synthesized compounds were screened for their preliminary in vitro antimicrobial activity against a panel of pathogenic strains of bacteria and fungi. Molecular docking and pharmacokinetic study were carried out for the prepared compounds. The cytotoxicity of the synthesized compounds was tested at different concentrations using bioassay of S. pombe cells at the cellular level. The effect of synthesized compounds on the DNA integrity of S. pombe was observed on agarose gel. Compounds 6d, 6e, 6g, 6h, 6j and 6n exhibited excellent antimicrobial potency as compared to the standard drugs (i.e Ampicillin, Norfloxacin, Chloramphenicol, Ciprofloxacin). Compounds 6d, 6e, 6g, 6k and 6n were found to have significant antifungal activity as compared to griseofulvin. Compounds 6f, 6i, 6k, 61 were found very less cytotoxic, while compounds 6d, 6e, 6g, 6h were found to exhibit maximum toxicity. The rest of the synthesized compounds were found to be moderately toxic. (C) 2016 Published by Elsevier Masson SAS.