Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: continued optimization of an MLPCN probe molecule.

Melancon BJ, Poslusney MS, Gentry PR, Tarr JC, Sheffler DJ, Mattmann ME, Bridges TM, Utley TJ, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Wood MR
Bioorg Med Chem Lett. 2013 23 (2): 412-6

PMID: 23237839 · PMCID: PMC3534865 · DOI:10.1016/j.bmcl.2012.11.092

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 M(1) 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 M(1) receptor was also maintained.

Copyright © 2012 Elsevier Ltd. All rights reserved.

MeSH Terms (6)

Inhibitory Concentration 50 Isatin Molecular Probes Molecular Structure Monoamine Oxidase Inhibitors Receptor, Muscarinic M1

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