Ontology highlight
ABSTRACT:
SUBMITTER: Capstick RA
PROVIDER: S-EPMC11318023 | biostudies-literature | 2024 Aug
REPOSITORIES: biostudies-literature
Capstick Rory A RA Bollinger Sean R SR Engers Julie L JL Long Madeline F MF Chang Sichen S Luscombe Vincent B VB Rodriguez Alice L AL Niswender Colleen M CM Bridges Thomas M TM Boutaud Olivier O Conn P Jeffrey PJ Engers Darren W DW Lindsley Craig W CW Temple Kayla J KJ
ACS medicinal chemistry letters 20240703 8
This Letter details our efforts to develop novel tricyclic muscarinic acetylcholine receptor subtype 4 (M<sub>4</sub>) positive allosteric modulator (PAM) scaffolds with improved pharmacological properties. This endeavor involved a "tie-back" strategy to replace the 3-amino-5-chloro-4,6-dimethylthieno[2,3-<i>b</i>]pyridine-2-carboxamide core, which led to the discovery of two novel tricyclic cores: an 8-chloro-9-methylpyrido[3',2':4,5]thieno[3,2-<i>d</i>]pyrimidin-4-amine core and 8-chloro-7,9-d ...[more]