Development of a prostaglandin D2 receptor antagonist: discovery of a new chemical lead
摘要:
A series of N-(p-alkoxy)benzoyl-5-methoxy-2-methylindole-3-acetic acids and N-(p-butoxy)benzoyl-2-methylindole-4-acetic acid were discovered as new chemical leads for a prostaglandin D-2 (PGD(2)) receptor antagonist. Most of them exhibited PGD(2) receptor binding and blocked cyclic adenosine 3',5'-monophosphate (cAMP) formation in vitro. In particular, 2-methylindole-4-acetic acid analog 1 showed markedly increased receptor affinity and cAMP antagonist activity. Chemistry and structure activity relationship (SAR) data are also presented. (c) 2005 Elsevier SAS. All rights reserved.
Development of a prostaglandin D2 receptor antagonist: discovery of a new chemical lead
摘要:
A series of N-(p-alkoxy)benzoyl-5-methoxy-2-methylindole-3-acetic acids and N-(p-butoxy)benzoyl-2-methylindole-4-acetic acid were discovered as new chemical leads for a prostaglandin D-2 (PGD(2)) receptor antagonist. Most of them exhibited PGD(2) receptor binding and blocked cyclic adenosine 3',5'-monophosphate (cAMP) formation in vitro. In particular, 2-methylindole-4-acetic acid analog 1 showed markedly increased receptor affinity and cAMP antagonist activity. Chemistry and structure activity relationship (SAR) data are also presented. (c) 2005 Elsevier SAS. All rights reserved.