Fused heterocyclic M1 positive allosteric modulators.
Fused aromatics such as naphthalene were identified as highly potent and CNS penetrant M(1) positive allosteric modulators during an SAR study to replace the phenyl B-ring linkage.
Department of Medicinal Chemistry, Merck Research Laboratories, Sumneytown Pike, PO Box 4, West Point, PA 19486, USA. scott_d_kuduk@merck.com
Scott D
SD
Kuduk
Christina N
CN
Di Marco
Victoria
V
Cofre
William J
WJ
Ray
Lei
L
Ma
Marion
M
Wittmann
Matthew A
MA
Seager
Kenneth A
KA
Koeplinger
Charles D
CD
Thompson
George D
GD
Hartman
Mark T
MT
Bilodeau
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000097:blood / Q000134:cerebrospinal fluid; D000494:Allosteric Regulation / Q000187:drug effects; D000818:Animals; D002264:Carboxylic Acids / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D015394:Molecular Structure; D009284:Naphthols / Q000737:chemistry* / Q000494:pharmacology; D015363:Quinolones / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D043643:Receptor, Muscarinic M1 / Q000378:metabolism*; D013329:Structure-Activity Relationship
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D002264:Carboxylic Acids; D009284:Naphthols; D015363:Quinolones; D043643:Receptor, Muscarinic M1