脱氧糖作为抗结核药物和α-甘露糖苷酶抑制剂。
Deoxysugars as antituberculars and alpha-mannosidase inhibitors.
作者信息
Kashyap Vivek, Sharma Smriti, Singh Vinayak, Sharma Sandeep K, Saquib Mohammad, Srivastava Ranjana, Shaw Arun K
机构信息
Division of Microbiology, CSIR-Central Drug Research Institute, Janakipuram Extension, Lucknow, India.
Process & Medicinal Chemistry Division, CSIR Central Drug Research Institute, Janakipuram Extension, Lucknow, India.
出版信息
Antimicrob Agents Chemother. 2014 Jun;58(6):3530-2. doi: 10.1128/AAC.02715-13. Epub 2014 Mar 31.
Abstract
A promising modified sugar molecule was identified which was active against multidrug-resistant (MDR) strains of Mycobacterium tuberculosis, suggesting involvement of a new target. The compound was demonstrated to be bactericidal, inhibited the growth of M. tuberculosis in mice, and targeted alpha-mannosidase as a competitive inhibitor with a Ki value of 353.9 μM.
摘要
一种有前景的修饰糖分子被鉴定出来，它对结核分枝杆菌的多重耐药（MDR）菌株具有活性，这表明涉及一个新的靶点。该化合物被证明具有杀菌作用，能抑制小鼠体内结核分枝杆菌的生长，并以α-甘露糖苷酶为靶点，作为竞争性抑制剂，其Ki值为353.9μM。
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