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 :
A series of N-(p-alkoxy)benzoyl-2-methylindole-4-acetic acids were synthesized and evaluated for prostaglandin D2 (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 PGD2-induced increase of microvascular permeability. Structure–activity relationship (SAR) data are presented.
Keywords :
Antagonist.* Corresponding author. Tel.: +81-75-961-1151 , fax: +81-75-962-9314 , DP receptor , e-mail: torisu@ono.co.jp , Prostaglandin
