High-throughput screening for inhibitors of Mycobacterium tuberculosis H37Rv.

High-throughput screening for inhibitors of Mycobacterium tuberculosis H37Rv.
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DOI:
10.1016/j.tube.2009.05.008
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发表时间:
2009-09
期刊:
Tuberculosis (Edinburgh, Scotland)
影响因子:
--
通讯作者:
White EL
White EL
中科院分区:
其他
文献类型:
--
作者:
Ananthan S;Faaleolea ER;Goldman RC;Hobrath JV;Kwong CD;Laughon BE;Maddry JA;Mehta A;Rasmussen L;Reynolds RC;Secrist JA 3rd;Shindo N;Showe DN;Sosa MI;Suling WJ;White EL

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迫切需要发现和开发新的抗结核药物,以新的生化途径为靶点,治疗耐药形式的疾病。解决这一需求的一种方法是通过针对整个细菌高通量筛选与药物相关的文库,以发现各种新的活性支架,这些支架将刺激新的生物研究和药物发现。通过结核病抗菌剂获取和协调机制(www.taacf.org),针对结核分枝杆菌H37Rv菌株筛选了一个大型的、与医学相关的化学药库。本文报道了该化合物的筛选方法和结果的药物化学分析。
There is an urgent need for the discovery and development of new antitubercular agents that target new biochemical pathways and treat drug resistant forms of the disease. One approach to addressing this need is through high throughput screening of medicinally relevant libraries against the whole bacterium in order to discover a variety of new, active scaffolds that will stimulate new biological research and drug discovery. Through the Tuberculosis Antimicrobial Acquisition and Coordinating Facility (www.taacf.org), a large, medicinally relevant chemical library was screened against M. tuberculosis strain H37Rv. The screening methods and a medicinal chemistry analysis of the results are reported herein.
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