196520-11-3Relevant academic research and scientific papers
Carboxylic acid derivatives having fused rings
-
, (2008/06/13)
The present invention provides a medicament exhibiting excellent retinoic acid receptor agonism. A Carboxylic acid derivative having a fused ring which is represented by the following formula or a pharmacologically acceptable salt thereof: {wherein the symbol represents a single bond or a double bond; X, Y, Z, P, Q, U, V and W are each a group represented by the formula: -O- or -S-, or a group represented by the formula: [wherein Rk (k: 1 to 8) is hydrogen, halogeno, optionally substituted lower alkyl or the like, with either of R7 and R8 being a group represented by the formula: (wherein A and B are each independently an optionally substituted aromatic hydrocarbon ring or an optionally substituted unsaturated heterocycle; and D is optionally protected carboxyl)]}.
Discovery of novel and potent retinoic acid receptor α agonists: Syntheses and evaluation of benzofuranyl-pyrrole and benzothiophenyl-pyrrole derivatives
Yoshimura, Hiroyuki,Kikuchi, Kouichi,Hibi, Shigeki,Tagami, Katsuya,Satoh, Takashi,Yamauchi, Toshihiko,Ishibahi, Akira,Tai, Kenji,Hida, Takayuki,Tokuhara, Naoki,Nagai, Mitsuo
, p. 2929 - 2937 (2007/10/03)
In the course of our studies on retinoic acid receptor (RAR) agonists, we have designed and synthesized a series of benzofuran and benzothiophene derivatives. Some of these compounds (1a,b,e,f,j) markedly inhibited LPS- induced B-lymphocyte proliferation and exerted RARα selectivity. One of them, 4-[5-(4,7-dimethylbenzofuran-2-yl)pyrrol-2-yl]benzoic acid (1b), when orally administered significantly inhibited mouse antibody production and delayed type hypersensitivity (DTH) responses from a dose of 0.1 mg/kg.
