Combinatorial synthesis of 3-(amidoalkyl) and 3-(aminoalkyl)-2-arylindole derivatives: discovery of potent ligands for a variety of G-protein coupled receptors.
Preparation and screening of mixture libraries based on a 2-arylindole scaffold resulted in the discovery of potent ligands for a variety of G-protein coupled receptors.
Willoughby
Christopher A
CA
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. christopher_willoughby@merck.com
Hutchins
Steven M
SM
Rosauer
Keith G
KG
Dhar
Madhumeeta J
MJ
Chapman
Kevin T
KT
Chicchi
Gary G
GG
Sadowski
Sharon
S
Weinberg
David H
DH
Patel
Smita
S
Malkowitz
Lorraine
L
Di Salvo
Jerry
J
Pacholok
Stephen G
SG
Cheng
Kang
K
D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000588:Amines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001667:Binding, Competitive / Q000187:drug effects; D020650:Combinatorial Chemistry Techniques; D004353:Drug Evaluation, Preclinical; D019204:GTP-Binding Proteins; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008024:Ligands; D011956:Receptors, Cell Surface / Q000378:metabolism*; D019707:Receptors, Chemokine / Q000378:metabolism; D011985:Receptors, Serotonin / Q000378:metabolism; D018039:Receptors, Tachykinin / Q000378:metabolism; D013329:Structure-Activity Relationship
D000577:Amides; D000588:Amines; D007211:Indoles; D008024:Ligands; D011956:Receptors, Cell Surface; D019707:Receptors, Chemokine; D011985:Receptors, Serotonin; D018039:Receptors, Tachykinin; D019204:GTP-Binding Proteins