10.1016/j.farmac.2004.08.003
The study focuses on the synthesis and preliminary pharmacological evaluation of a new series of muscarinic antagonists derived from 2,2-diphenyl-2-ethylthio-acetic acid esters. These compounds were designed to probe the binding site cavity of muscarinic receptors, which are found in the central and peripheral nervous system and play a crucial role in various vital functions. The researchers aimed to enhance the potency and selectivity of these antagonists by decorating the parent molecules with linkers of different lengths, carrying an amino group to potentially interact with an anionic function outside the recognition site of the receptor. The chemicals used in the study included 2,2-diphenyl-2-ethylthio-acetic acid esters, various chloramines, amino alcohols, and other organic compounds to synthesize the new series of compounds (3–20). The purpose of these chemicals was to create probes that could interact with the muscarinic receptor subtypes and potentially lead to the development of more selective and potent therapeutic agents for pathologies such as smooth muscle hyperactivity and neurodegenerative diseases. However, the study found that while the new compounds showed some increase in affinity, they lacked subtype selectivity and did not meet the expected outcomes, leading to the identification of a series of compounds with a peculiar pharmacological profile.