Publications by authors named "Jeffrey J Adams"
ACS Chem Neurosci
April 2017
Article Synopsis
- Recent studies indicate that the M muscarinic acetylcholine receptor could be a promising target for treating Alzheimer's and schizophrenia, but initial drug discovery attempts were unsuccessful in achieving selectivity for M activation.
- Researchers are now focusing on allosteric modulators, known as positive allosteric modulators (PAMs), to selectively activate M receptors, although some PAMs can cause adverse effects that limit their use.
- The study reveals that within a series of indole-based M PAMs, a novel compound was discovered that does not induce adverse effects, despite having a similar molecular profile to another PAM that does, emphasizing the need for in vivo testing to identify effective and safe treatments.
Bioorg Med Chem Lett
August 2016
Article Synopsis
- The letter details the ongoing chemical optimization of the VU0453595 series, which are M1 positive allosteric modulators (PAMs) used for central nervous system (CNS) targets.
- Researchers explored new 5,6- and 6,6-heterobicyclic structures to replace the original core in VU453595, which led to compounds with improved potency and better CNS distribution.
- This research introduced a variety of new chemical structures for M1 PAMs that lack hydrogen-bond donors, significantly enhancing the structural diversity available for further CNS studies.
