Title of article :
Discovery of a new class of potent, selective, and orally active prostaglandin D2 receptor antagonists Original Research Article
Author/Authors :
Kazuhiko Torisu، نويسنده , , Kaoru Kobayashi، نويسنده , , Maki Iwahashi، نويسنده , , Yoshihiko Nakai، نويسنده , , Takahiro Onoda، نويسنده , , Toshihiko Nagase، نويسنده , , Isamu Sugimoto، نويسنده , , Yutaka Okada، نويسنده , , Ryoji Matsumoto، نويسنده , , Fumio Nanbu، نويسنده , , Shuichi Ohuchida، نويسنده , , Hisao Nakai، نويسنده , , Masaaki Toda، نويسنده ,
Abstract :
The process of discovering a series of N-(p-alkoxy)benzoyl-2-methylindole-4-acetic acid analogs is presented since these compounds represent a new class of potent, selective, and orally active prostaglandin D2 (PGD2) receptor antagonists. Most of these compounds exhibit strong PGD2 receptor binding and PGD2 receptor antagonism in cAMP formation assays. When given orally, these new antagonists dramatically suppress allergic inflammatory responses, such as the PGD2-induced or OVA-induced increase of vascular permeability. Structure–activity relationship (SAR) data are also discussed.
