191212-86-9Relevant articles and documents
Design, synthesis, and evaluation of novel anti-trypanosomal compounds
Lepovitz, Lance T.,Martin, Stephen F.,Meis, Alan R.,Mensa-Wilmot, Kojo,Pham, Alexandra,Thomas, Sarah M.,Wiedeman, Justin
, (2020/03/25)
Human African trypanosomiasis (HAT) is a deadly neglected tropical disease caused by the protozoan parasite Trypanosoma brucei. During the course of screening a collection of diverse nitrogenous heterocycles, we discovered two novel compounds that contain the tetracyclic core of the Yohimbine and Corynanthe alkaloids, were potent inhibitors of T. brucei proliferation and T. brucei methionyl-tRNA synthetase (TbMetRS) activity. Inspired by these key findings, we prepared several novel series of hydroxyalkyl δ-lactam, δ-lactam, and piperidine analogs and tested their anti-trypanosomal activity. A number of inhibitors were more potent against T. brucei than these initial hits with one hydroxyalkyl δ-lactam derivative being 25-fold more effective in our assay. Surprisingly, most of these active compounds failed to inhibit TbMetRS. This work underscores the importance of verifying, irrespective of close structural similarities, that new compounds designed from a lead with a known biological target engage the putative binding site.
Cyclic amine derivative and pharmaceutical use thereof
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Paragraph 0301, (2016/10/09)
The purpose of the present invention is to provide a compound that exerts a strong analgesic action against on pain, in particular, against neuropathic pain and/or fibromyalgia syndrome. The present invention provides a cyclic amine derivative represented by chemical formula, a prodrug thereof or a pharmaceutically acceptable salt thereof.
Substituted Benzamide Compounds
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Page/Page column 140, (2012/04/04)
Substituted benzamide compounds corresponding to formula (I) in which R5, R6, R7, R8, a, b, c, d, t, D and X have defined meanings, a process for their preparation, pharmaceutical compositions comprising such compounds, and a method of using such compounds to treat pain and other conditions mediated at least in part via the bradykinin 1 receptor.