天然产物先导药物发现：6-氰基-5-甲氧基吲哚并[2,3-a]咔唑类配体的分离、合成及作为抗菌剂的生物评价。
Natural product leads for drug discovery: isolation, synthesis and biological evaluation of 6-cyano-5-methoxyindolo[2,3-a]carbazole based ligands as antibacterial agents.
机构信息
Drug Discovery Program, Department of Medicinal Chemistry and Pharmacognosy, University of Illinois at Chicago, 833 S. Wood Street, Chicago, USA.
出版信息
Bioorg Med Chem. 2009 Oct 15;17(20):7126-30. doi: 10.1016/j.bmc.2009.08.061. Epub 2009 Sep 4.
Abstract
Indolo[2,3-a]carbazole based inhibitors were synthesized from readily available indigo via a seven-step linear synthetic sequence with a moderate overall yield. The inhibitors were selectively and readily functionalized at the nitrogen on the indole portion of the carbazole unit. The synthesized analogs displayed moderate inhibitory activities toward Bacillus anthracis and Mycobacterium tuberculosis, indicating that indolo[2,3-a]carbazoles could serve as promising leads in the development of new drugs to combat anthrax and tuberculosis infections.
摘要
基于吲哚并[2,3-a]咔唑的抑制剂是通过具有中等总产率的七步线性合成序列，从易得的靛蓝合成的。抑制剂可在咔唑单元的吲哚部分的氮上选择性且容易地进行官能化。合成的类似物对炭疽芽孢杆菌和结核分枝杆菌表现出中等抑制活性，表明吲哚并[2,3-a]咔唑可作为开发用于治疗炭疽和结核病感染的新药的有前途的先导化合物。
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