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 discovery for highly potent prostaglandin D2 (PGD2) receptor antagonists is reported. A series of N-(p-alkoxy)benzoyl-2-methylindole-4-acetic acids were synthesized and identified as a new class of selective PGD2 receptor antagonists. Most of them exhibited strong PGD2 receptor antagonism in binding studies and the cAMP formation assay. The structure–activity relationships (SAR), including subtype selectivity of the synthesized compounds, are also discussed.
