两种新型利福布丁类似物对耐多药结核分枝杆菌的体外活性强。
Strong in vitro activities of two new rifabutin analogs against multidrug-resistant Mycobacterium tuberculosis.
机构信息
Instituto Universitario de Química Organometálica Enrique Moles, Unidad Asociada al C.S.I.C., Universidad de Oviedo, c/ Julián Clavería 8, 33006 Oviedo, Spain.
出版信息
Antimicrob Agents Chemother. 2010 Dec;54(12):5363-5. doi: 10.1128/AAC.00149-10. Epub 2010 Sep 20.
Abstract
Two new rifabutin analogs, RFA-1 and RFA-2, show high in vitro antimycobacterial activities against Mycobacterium tuberculosis. MIC values of RFA-1 and RFA-2 were ≤0.02 μg/ml against rifamycin-susceptible strains and 0.5 μg/ml against a wide selection of multidrug-resistant strains, compared to ≥50 μg/ml for rifampin and 10 μg/ml for rifabutin. Molecular dynamic studies indicate that the compounds may exert tighter binding to mutants of RNA polymerase that have adapted to the rifamycins.
摘要
两种新的利福布汀类似物，RFA-1 和 RFA-2，对结核分枝杆菌显示出很高的体外抗分枝杆菌活性。与利福平（≥50μg/ml）和利福布丁（10μg/ml）相比，RFA-1 和 RFA-2 的 MIC 值对利福平敏感株为≤0.02μg/ml，对多种耐药株为 0.5μg/ml。分子动力学研究表明，这些化合物可能与适应利福霉素的 RNA 聚合酶突变体有更紧密的结合。
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本文引用的文献
1
New rifabutin analogs: synthesis and biological activity against Mycobacterium tuberculosis.
Bioorg Med Chem Lett. 2006 Nov 15;16(22):5717-22. doi: 10.1016/j.bmcl.2006.08.090. Epub 2006 Sep 20.
2
The global alliance for tuberculosis drug development--accomplishments and future directions.
Clin Chest Med. 2005 Jun;26(2):341-7, vii. doi: 10.1016/j.ccm.2005.02.008.
3
New drugs for tuberculosis: current status and future prospects.
Clin Chest Med. 2005 Jun;26(2):327-40, vii. doi: 10.1016/j.ccm.2005.02.013.
4
Rifamycin-mode of action, resistance, and biosynthesis.
Chem Rev. 2005 Feb;105(2):621-32. doi: 10.1021/cr030112j.
5
Structural, functional, and genetic analysis of sorangicin inhibition of bacterial RNA polymerase.
EMBO J. 2005 Feb 23;24(4):674-82. doi: 10.1038/sj.emboj.7600499. Epub 2005 Feb 3.
6
NMR spectroscopic analysis of new spiro-piperidylrifamycins.
Magn Reson Chem. 2005 Apr;43(4):269-82. doi: 10.1002/mrc.1545.
7
Antiretroviral drugs for tuberculosis control in the era of HIV/AIDS.
Science. 2003 Sep 12;301(5639):1535-7. doi: 10.1126/science.1086845. Epub 2003 Aug 14.
8
The growing burden of tuberculosis: global trends and interactions with the HIV epidemic.
Arch Intern Med. 2003 May 12;163(9):1009-21. doi: 10.1001/archinte.163.9.1009.
9
Worldwide incidence of multidrug-resistant tuberculosis.
J Infect Dis. 2002 Apr 15;185(8):1197-202. doi: 10.1086/339818. Epub 2002 Apr 1.
10
Detection of rifampicin-resistance mutations in Mycobacterium tuberculosis.
Lancet. 1993 Mar 13;341(8846):647-50. doi: 10.1016/0140-6736(93)90417-f.
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