Author/Authors :
Masaki Asada، نويسنده , , Tetsuo Obitsu، نويسنده , , Toshihiko Nagase، نويسنده , , Isamu Sugimoto، نويسنده , , Yoshiyuki Yamaura، نويسنده , , Kazutoyo Sato، نويسنده , , Masami Narita، نويسنده , , Shuichi Ohuchida، نويسنده , , Hisao Nakai، نويسنده , , Masaaki Toda، نويسنده ,
Abstract :
A series of acrylic acids and their structurally related compounds were evaluated for their binding affinity to four EP receptor subtypes (EP1-4). Starting from the initial hit 3, which was discovered in our in-house library, compounds 4 and 5 were identified as new chemical leads as candidates for further optimization towards a selective EP3 receptor antagonist. The identification process of these compounds and their pharmacokinetic profiles are presented.
Keywords :
Prostaglandin , EP3 receptor , Pyrazole , Antagonist
