Isatin replacements applied to the highly selective, muscarinic M 1 PAM ML137: Continued optimization of an MLPCN probe molecule
This Letter describes the continued optimization of an MLPCN probe molecule (ML137) with a focused effort on the replacement/modification of the isatin moiety present in this highly selective M1 PAM. A diverse range of structures were validated as viable replacements for the isatin, many of which engendered sizeable improvements in their ability to enhance the potency and efficacy of acetylcholine when compared to ML137. Muscarinic receptor subtype selectivity for the M1 receptor was also maintained.
Melancon, Bruce J.,Poslusney, Michael S.,Gentry, Patrick R.,Tarr, James C.,Sheffler, Douglas J.,Mattmann, Margrith E.,Bridges, Thomas M.,Utley, Thomas J.,Daniels, J. Scott,Niswender, Colleen M.,Conn, P. Jeffrey,Lindsley, Craig W.,Wood, Michael R.
p. 412 - 416
(2013/02/23)
SUBSTITUTED 4-(1H~PYRAZOL-4.YL)BENZYL ANALOGUES AS POSITIVE ALLOSTERIC MODULATORS OF MACHR M1 RECEPTORS
In one aspect, the invention relates to substituted 4-(lH-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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Paragraph 00509; 00641; 00642
(2013/07/25)
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