|
|||||
|
|
Discovery of orally active prostaglandin D2 receptor antagonists |
|
| Authors: | Torisu Kazuhiko Kobayashi Kaoru Iwahashi Maki Nakai Yoshihiko Onoda Takahiro Nagase Toshihiko Sugimoto Isamu Okada Yutaka Matsumoto Ryoji Nanbu Fumio Ohuchida Shuichi Nakai Hisao Toda Masaaki |
| Affiliation: | Minase Research Institute, Ono Pharmaceutical Co., Ltd, Shimamoto, Osaka, Mishima 618-8585, Japan. torisu@ono.co.jp |
| Abstract: | A series of N-(p-alkoxy)benzoyl-2-methylindole-4-acetic acids were synthesized and evaluated for prostaglandin D(2) (DP) receptor affinity and antagonist activity. Some of them exhibited strong receptor binding and were potent in the cAMP formation assays. These antagonists also suppressed allergic inflammatory responses such as the PGD(2)-induced increase of microvascular permeability. Structure-activity relationship (SAR) data are presented. |
| Keywords: | |
| 本文献已被 PubMed 等数据库收录！ | |