3-三氮烯吲哚对结核分枝杆菌和鸟分枝杆菌的体外活性
In Vitro Activity of 3-Triazeneindoles against Mycobacterium tuberculosis and Mycobacterium avium.
作者信息
Nikonenko Boris V, Kornienko Albert, Majorov Konstantin, Ivanov Pavel, Kondratieva Tatiana, Korotetskaya Maria, Apt Alexander S, Salina Elena, Velezheva Valeriya
机构信息
Central Institute for Tuberculosis, Moscow, Russia TB-Stopper, Skolkovo, Moscow, Russia
A. N. Nesmeyanov Institute of Organoelement Compounds of the Russian Academy of Sciences, Moscow, Russia.
出版信息
Antimicrob Agents Chemother. 2016 Sep 23;60(10):6422-4. doi: 10.1128/AAC.00998-16. Print 2016 Oct.
Abstract
Among 230 target-synthesized indole-based compounds, seven 3-triazenoindoles showed MICs of 0.2 to 0.5 μg/ml against Mycobacterium tuberculosis strain H37Rv and isoniazid-resistant human isolate CN-40. The TU112 compound was active also against a dormant form of M. tuberculosis Some of these triazenoindoles were active against Mycobacterium avium, with MICs of 0.05 to 0.5 μg/ml. The selectivity indices (SI) for M. tuberculosis and M. avium were significantly higher than 10, making these compounds acceptable for the next testing step.
摘要
在230种靶向合成的吲哚类化合物中，7种3-三氮烯吲哚对结核分枝杆菌H37Rv菌株和耐异烟肼的人分离株CN-40的最低抑菌浓度（MIC）为0.2至0.5μg/ml。TU112化合物对结核分枝杆菌的休眠形式也有活性。其中一些三氮烯吲哚对鸟分枝杆菌有活性，MIC为0.05至0.5μg/ml。针对结核分枝杆菌和鸟分枝杆菌的选择性指数（SI）显著高于10，使得这些化合物可进入下一步测试。
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本文引用的文献
1
Synthesis and antituberculosis activity of indole-pyridine derived hydrazides, hydrazide-hydrazones, and thiosemicarbazones.
Bioorg Med Chem Lett. 2016 Feb 1;26(3):978-985. doi: 10.1016/j.bmcl.2015.12.049. Epub 2015 Dec 17.
2
Design, chemical synthesis of 3-(9H-fluoren-9-yl)pyrrolidine-2,5-dione derivatives and biological activity against enoyl-ACP reductase (InhA) and Mycobacterium tuberculosis.
Eur J Med Chem. 2013;70:37-48. doi: 10.1016/j.ejmech.2013.09.041. Epub 2013 Oct 2.
3
New 2-thiopyridines as potential candidates for killing both actively growing and dormant Mycobacterium tuberculosis cells.
Antimicrob Agents Chemother. 2014;58(1):55-60. doi: 10.1128/AAC.01308-13. Epub 2013 Oct 14.
4
Preliminary structure-activity relationships and biological evaluation of novel antitubercular indolecarboxamide derivatives against drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.
J Med Chem. 2013 May 23;56(10):4093-103. doi: 10.1021/jm4003878. Epub 2013 May 3.
5
Identification of SQ609 as a lead compound from a library of dipiperidines.
Bioorg Med Chem Lett. 2011 Sep 15;21(18):5353-7. doi: 10.1016/j.bmcl.2011.07.015. Epub 2011 Jul 14.
6
In vitro antimicrobial activities of capuramycin analogues against non-tuberculous mycobacteria.
J Antimicrob Chemother. 2010 Dec;65(12):2590-7. doi: 10.1093/jac/dkq372. Epub 2010 Oct 14.
7
Host genetics in granuloma formation: human-like lung pathology in mice with reciprocal genetic susceptibility to M. tuberculosis and M. avium.
PLoS One. 2010 May 6;5(5):e10515. doi: 10.1371/journal.pone.0010515.
8
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Antimicrob Agents Chemother. 2004 Dec;48(12):4550-5. doi: 10.1128/AAC.48.12.4550-4555.2004.
9
Novel pyridazino[4,3-b]indoles with dual inhibitory activity against Mycobacterium tuberculosis and monoamine oxidase.
J Med Chem. 2004 Jun 17;47(13):3455-61. doi: 10.1021/jm030479g.
10
Different innate ability of I/St and A/Sn mice to combat virulent Mycobacterium tuberculosis: phenotypes expressed in lung and extrapulmonary macrophages.
Infect Immun. 2003 Feb;71(2):697-707. doi: 10.1128/IAI.71.2.697-707.2003.
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