Inhibitors of Fumarylacetoacetate Hydrolase Domain Containing Protein 1 (FAHD1)
作者:Alexander K. H. Weiss、Richard Wurzer、Patrycia Klapec、Manuel Philip Eder、Johannes R. Loeffler、Susanne von Grafenstein、Stefania Monteleone、Klaus R. Liedl、Pidder Jansen-Dürr、Hubert Gstach
DOI:10.3390/molecules26165009
日期:——
domain containing protein 1 (FAHD1) acts as oxaloacetate decarboxylase in mitochondria, contributing to the regulation of the tricarboxylic acid cycle. Guided by a high-resolution X-ray structure of FAHD1 liganded by oxalate, the enzymatic mechanism of substrate processing is analyzed in detail. Taking the chemical features of the FAHD1 substrate oxaloacetate into account, the potential inhibitor structures
含有 FAH 结构域的蛋白 1 (FAHD1) 在线粒体中充当草酰乙酸脱羧酶,有助于三羧酸循环的调节。以草酸配体的 FAHD1 的高分辨率 X 射线结构为指导,详细分析了底物处理的酶促机制。考虑到 FAHD1 底物草酰乙酸的化学特征,推断出潜在的抑制剂结构。药物样支架的合成提供了第一代 FAHD1 抑制剂,其活性在低微摩尔 IC 50范围内。研究揭示了与底物竞争结合金属辅因子的结构,以及支架,它们可能具有与 FAHD1 的新结合模式。
1,3-Disubstituted 4-methyl-1H-pyrrole-2-carboxamides and their Use in Medicaments
申请人:Oberboersch Stefan
公开号:US20090137573A1
公开(公告)日:2009-05-28
1,3-disubstituted 4-methyl-1H-pyrrole-2-carboxamides corresponding to formula I
methods for their production, pharmaceutical compositions containing them, and the use thereof for noradrenalin receptor regulation, particularly for inhibiting noradrenalin reuptake, and/or for 5-HT receptor regulation, particularly for inhibiting 5-hydroxy tryptophan reuptake, and/or for opioid receptor regulation and/or for batrachotoxin (BTX) receptor regulation and/or for treating or inhibiting pain and other conditions.
Substituted 5,6,7,8-Tetrahydroimidazo[1,2-a]pyridin-2-ylamine Compounds and Their Use for Producing Drugs
申请人:Frank Robert
公开号:US20080300256A1
公开(公告)日:2008-12-04
Substituted 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-ylamine compounds corresponding to formula I, methods for the preparation thereof, pharmaceutical compositions containing said compounds, the use of said compounds for preparing pharmaceutical compositions and related treatment methods.