Southern Research Institute, 2000 Ninth Avenue South, Birmingham, AL 35205, USA.
Tuberculosis (Edinb). 2009 Sep;89(5):354-63. doi: 10.1016/j.tube.2009.07.006. Epub 2009 Sep 26.
There is an urgent need for the discovery and development of new antitubercular agents that target novel biochemical pathways and treat drug-resistant forms of the disease. One approach to addressing this need is through high-throughput screening of drug-like small molecule libraries against the whole bacterium in order to identify a variety of new, active scaffolds that will stimulate additional biological research and drug discovery. Through the Molecular Libraries Screening Center Network, the NIAID Tuberculosis Antimicrobial Acquisition and Coordinating Facility tested a 215,110-compound library against Mycobacterium tuberculosis strain H37Rv. A medicinal chemistry survey of the results from the screening campaign is reported herein.
迫切需要发现和开发针对新生化途径的新型抗结核药物，以治疗耐药形式的结核病。满足这一需求的一种方法是针对整个细菌进行高通量筛选类药性小分子文库，以鉴定各种新的、有效的支架，从而激发更多的生物学研究和药物发现。通过分子文库筛选中心网络，NIAID 结核抗菌药物获取和协调机构对结核分枝杆菌 H37Rv 菌株进行了 215110 化合物文库的测试。本文报道了此次筛选活动的药物化学调查结果。
