title: Evolution of novel tricyclic CRTh2 receptor antagonists from a (E)-2-cyano-3-(1H-indol-3-yl)acrylamide scaffold.
abstract: (E)-2-(3-(3-((3-Bromophenyl)amino)-2-cyano-3-oxoprop-1-en-1-yl)-1H-indol-1-yl)acetic acid (1) was discovered in a HTS campaign for CRTh2 receptor antagonists. An SAR around this hit could be established and representatives with interesting activity profiles were obtained. Ring closing tactics to convert this hit series into a novel 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole based CRTh2 receptor antagonist series is presented.
authors: Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, CH-4123 Allschwil, Switzerland.
authors: Anja
authors: A
authors: Valdenaire
authors: Julien
authors: J
authors: Pothier
authors: Dorte
authors: D
authors: Renneberg
authors: Markus A
authors: MA
authors: Riederer
authors: Oliver
authors: O
authors: Peter
authors: Xavier
authors: X
authors: Leroy
authors: Carmela
authors: C
authors: Gnerre
authors: Heinz
authors: H
authors: Fretz
mesh_terms: D000178:Acrylamides / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D006801:Humans; D007211:Indoles / Q000737:chemistry* / Q000494:pharmacology*; D008958:Models, Molecular; D051381:Rats; D011971:Receptors, Immunologic / Q000037:antagonists & inhibitors*; D011982:Receptors, Prostaglandin / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D000178:Acrylamides; D007211:Indoles; D011971:Receptors, Immunologic; D011982:Receptors, Prostaglandin; C036293:prostaglandin D2 receptor