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通过改进方案合成的N-[(1-甲基-1H-吲哚-3-基)亚甲基]胺的抗菌、冠瘿瘤抑制和细胞毒性测定

Antimicrobial, crown gall tumor inhibitory and cytotoxicity assays of N-[(1-methyl-1H-indole-3-yl)methylene]amines synthesized by an improved protocol.

作者信息

Singh Girija S, Al-kahraman Yasser M S A, Mpadi Disah, Yasinzai Masoom

机构信息

Chemistry Department, University of Botswana, Private Bag: 0022, Gaborone, Botswana.

出版信息

Med Chem. 2014 Jun;10(4):382-7. doi: 10.2174/15734064113099990035.

Abstract

The present paper reports an easy preparation of imines of N-methyl-1H-indole-3-carboxaldehyde by its condensation with alkyl and aromatic amines in ethanol without using any catalyst or dehydrating agent. The compounds have been screened for their antibacterial, antifungal, crown gall tumor inhibitory, and cytotoxic activities. As a major finding some of the compounds exhibited potential biological activity. The imine containing a 4-chlorophenyl group exhibits potential antitumor activity and brine shrimp lethality against crown gall tumor and brine shrimps, respectively. Furthermore, this imine containing a 4-chlorophenyl group also exhibits significant antifungal activity against Candida albicans fungal strains. The compound containing N-diphenylmethyl group has been observed most active against the Gram-positive bacteria.

摘要

本文报道了一种简便的制备N-甲基-1H-吲哚-3-甲醛亚胺的方法,该方法是在乙醇中使其与烷基胺和芳香胺缩合,无需使用任何催化剂或脱水剂。已对这些化合物的抗菌、抗真菌、冠瘿瘤抑制和细胞毒性活性进行了筛选。作为一项主要发现,一些化合物表现出潜在的生物活性。含有4-氯苯基的亚胺分别对冠瘿瘤和卤虫表现出潜在的抗肿瘤活性和卤虫致死性。此外,这种含有4-氯苯基的亚胺对白色念珠菌菌株也表现出显著的抗真菌活性。已观察到含有N-二苯甲基的化合物对革兰氏阳性菌活性最强。

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