In this review the various chemical structures of allosteric agonists and modulators of the muscarinic acetylcholine receptor subtype 1 (mAChR(1) or M-1) and their relevance for possible treatment of Alzheimer's disease (AD) are discussed. Furthermore, their design principles, common structural properties and their unique features with regard to structure-activity relationships (SARs), such as 'molecular switches' and 'steep/flat' SARs, are highlighted. M-1 bitopic ligands and hybrid molecules are also considered. All these differently designed M-1 allosteric modulators open exciting new paths in medicinal chemistry with most promising therapeutic opportunities to fight AD.
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