Nefzi Adel, Appel Jon, Arutyunyan Sergey, Houghten Richard A
Torrey Pines Institute for Molecular Studies, 3550 Genearl Atomocs Court, San Diego, CA 92121, USA.
Bioorg Med Chem Lett. 2009 Sep 1;19(17):5169-75. doi: 10.1016/j.bmcl.2009.07.010. Epub 2009 Jul 9.
Combinatorial chemistry offers a unique opportunity for the synthesis and screening of large numbers of compounds and significantly enhances the prospect of finding new drugs. Collaborative efforts with the Tuberculosis Antimicrobial Acquisition & Coordinating Facility (TAACF), have led to the identification of submicromolar novel antitubercular hits. Chiral pentaamines and bis-heterocyclic compounds with 90-100% inhibition against Mycobacterium tuberculosis strain H(37)R(v) were identified. Some of the identified compounds are more active than the existing drug ethambutol.
组合化学为大量化合物的合成和筛选提供了独特的机会，并显著提高了发现新药的前景。与结核病抗菌药物采购与协调机构（TAACF）的合作努力，已导致鉴定出亚微摩尔浓度的新型抗结核活性物质。已鉴定出对手结核分枝杆菌H(37)R(v)菌株具有90-100%抑制作用的手性五胺和双杂环化合物。一些鉴定出的化合物比现有药物乙胺丁醇更具活性。
