A novel series of 2-pyridyl-containing compounds as lysophosphatidic acid receptor antagonists: development of a nonhydrolyzable LPA3 receptor-selective antagonist
摘要:
A recently reported dual LPA(1)/LPA(3) receptor antagonist (1) has been modified so as to modulate the basicity, sterics, and dipole moment of the 2-pyridyl moiety. Additionally, the implications of installing nonhydrolyzable phosphate head group isosteres with regard to antagonist potency and selectivity at LPA receptors is described. This study has resulted in the development of the first nonhydrolyzable and presumably phosphatase-resistant LPA(3)-selective antagonist reported to date. (C) 2004 Elsevier Ltd. All rights reserved.
Photoredox-Catalyzed Hydroxymethylation of Heteroaromatic Bases
作者:Chelsea A. Huff、Ryan D. Cohen、Kevin D. Dykstra、Eric Streckfuss、Daniel A. DiRocco、Shane W. Krska
DOI:10.1021/acs.joc.6b00811
日期:2016.8.19
We report the development of a method for room-temperature C–H hydroxymethylation of heteroarenes. A key enabling advance in this work was achieved by implementing visible light photoredoxcatalysis that proved to be applicable to many classes of heteroarenes and tolerant of diverse functional groups found in druglike molecules.
A quinoline derivative represented by the following formula (1):
allows PPARα or γ which is an intranuclear transcription factor, to function strongly and is low in toxicity. By using this compound as an active ingredient, there can be provided a preventive or therapeutic agent for various diseases related to PPARα or γ.
A quinoline derivative represented by the following formula (1):
1
allows PPAR&agr; or &ggr; which is an intranuclear transcription factor, to function strongly and is low in toxicity. By using this compound as an active ingredient, there can be provided a preventive or therapeutic agent for various diseases related to PPAR&agr; or &ggr;.
A novel series of 2-pyridyl-containing compounds as lysophosphatidic acid receptor antagonists: development of a nonhydrolyzable LPA3 receptor-selective antagonist
作者:Brian H Heasley、Renata Jarosz、Karen M Carter、S Jenny Van、Kevin R Lynch、Timothy L Macdonald
DOI:10.1016/j.bmcl.2004.05.023
日期:2004.8
A recently reported dual LPA(1)/LPA(3) receptor antagonist (1) has been modified so as to modulate the basicity, sterics, and dipole moment of the 2-pyridyl moiety. Additionally, the implications of installing nonhydrolyzable phosphate head group isosteres with regard to antagonist potency and selectivity at LPA receptors is described. This study has resulted in the development of the first nonhydrolyzable and presumably phosphatase-resistant LPA(3)-selective antagonist reported to date. (C) 2004 Elsevier Ltd. All rights reserved.