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新型香豆素的抗结核活性。

Antitubercular activity of new coumarins.

机构信息

Universidade Federal de Alagoas, Campus Arapiraca, Rua Manoel Severino Barbosa s/n, Bonsucesso, Arapiraca, AL, Brazil.

出版信息

Chem Biol Drug Des. 2011 Jun;77(6):489-93. doi: 10.1111/j.1747-0285.2011.01120.x. Epub 2011 Apr 19.

Abstract

The present article describes a series of 21 N '-benzylidene-2-oxo-2H-chromene-3-carbohydrazides 4a-4v, which were synthesized and evaluated for their cell viabilities in non-infected and Mycobacterium bovis Bacillus Calmette-Guerin-infected macrophages. Subsequently, the non-cytotoxic compounds 4c, 4g, 4h, 4j, 4l and 4t were assessed against Mycobacterium tuberculosis ATCC 27294 using the microplate Alamar Blue assay and the activity expressed as the minimum inhibitory concentration in μg/mL. These compounds exhibited a significant activity (50-100 μg/mL) when compared to the first-line drugs, such as pyrazinamide (PZA >100 μg/mL). These results could be considered a good starting point for further studies to develop new lead compounds to treat multidrug-resistant tuberculosis.

摘要

本文描述了一系列 21 种 N-苯亚甲基-2-氧代-2H-色烯-3-甲酰肼 4a-4v,它们被合成并评估了它们在非感染和牛分枝杆菌卡介苗感染的巨噬细胞中的细胞活力。随后,使用微量板 Alamar Blue 测定法和以 μg/mL 表示的最小抑制浓度,评估了对结核分枝杆菌 ATCC 27294 无细胞毒性的化合物 4c、4g、4h、4j、4l 和 4t 的活性。与一线药物(如吡嗪酰胺(PZA>100μg/mL)相比,这些化合物表现出显著的活性(50-100μg/mL)。这些结果可以被认为是进一步研究开发治疗耐多药结核病的新先导化合物的良好起点。

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