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合成具有强大抗分枝杆菌和抗氧化功效的吲哚功能化异烟肼缀合物。

Synthesis of indole-functionalized isoniazid conjugates with potent antimycobacterial and antioxidant efficacy.

机构信息

Department of Chemistry, M. D. University, Rohtak, Haryana, 124001, India.

Department of Microbiology, Vallabhbhai Patel Chest Institute, University of Delhi, Delhi, 110007, India.

出版信息

Future Med Chem. 2024;16(17):1731-1747. doi: 10.1080/17568919.2024.2379240. Epub 2024 Jul 23.

Abstract

Developing potent medicinal alternates for tuberculosis (TB) is highly desirable due to the advent of drug-resistant lethal TB strains. Novel indole-isoniazid integrates have been synthesized with promising antimycobacterial action against the strain, and the nitro analogs and show the highest efficacy with a minimum inhibitory concentration of 1.25 μg/ml. The molecular docking studies against support the experimental findings. Indole conjugates display remarkable radical quenching efficiency, and compounds and demonstrate maximum IC values of 50.19 and 52.45 μg/ml, respectively. Pharmacokinetic analysis anticipated appreciable druggability for the title compounds. The notable bioaction of the indole-isoniazid templates projects them as potential lead in developing anti-TB medications with synergetic antioxidant action.

摘要

由于耐药性致命结核菌株的出现,开发有效的治疗结核病(TB)的替代药物是非常必要的。新型吲哚异烟肼整合物已经被合成出来,具有针对该菌株的有前途的抗分枝杆菌作用,并且硝基类似物 和 显示出最高的疗效,最低抑菌浓度为 1.25μg/ml。针对 的分子对接研究支持了实验结果。吲哚缀合物显示出显著的自由基猝灭效率,化合物 和 分别表现出最大的 IC 值 50.19 和 52.45μg/ml。药代动力学分析预计这些标题化合物具有良好的成药性。吲哚异烟肼模板的显著生物活性将其作为开发具有协同抗氧化作用的抗结核病药物的潜在先导化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/20d2/11457681/296b2eaff518/IFMC_A_2379240_UF0001_C.jpg

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