Poslusney, Michael S.; Melancon, Bruce J.; Gentry, Patrick R.; Sheffler, Douglas J.; Bridges, Thomas M.; Utley, Thomas J.; Daniels, J. Scott; Niswender, Colleen M.; Conn, P. Jeffrey; Lindsley, Craig W.; Wood, Michael R. published the artcile< Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: The continued optimization of an MLPCN probe molecule>, Related Products of 1046832-21-6, the main research area is spirocycle preparation SAR human rat muscarinic M1 receptor selectivity; pos allosteric modulator SAR spirocycle MLPCN probe mol.
This Letter describes the further optimization of an MLPCN probe mol. (ML137) through the introduction of 5- and 6-membered spirocycles in place of the isatin ketone. Interestingly divergent structure-activity relationships, when compared to earlier M1 PAMs, are presented. These novel spirocycles, e.g. I, possess improved efficacy relative to ML137, while also maintaining high selectivity for the human and rat muscarinic M1 receptor subtype.
Bioorganic & Medicinal Chemistry Letters published new progress about Homo sapiens. 1046832-21-6 belongs to class pyrazoles-derivatives, and the molecular formula is C11H19BN2O2, Related Products of 1046832-21-6.
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