Structure-activity relationships of constrained phenylethylamine ligands for the serotonin 5-HT2 receptors.

ABSTRACT: Serotonergic ligands have proven effective drugs in the treatment of migraine, pain, obesity, and a wide range of psychiatric and neurological disorders. There is a clinical need for more highly 5-HT2 receptor subtype-selective ligands and the most attention has been given to the phenethylamine class. Conformationally constrained phenethylamine analogs have demonstrated that for optimal activity the free lone pair electrons of the 2-oxygen must be oriented syn and the 5-oxygen lone pairs anti relative to the ethylamine moiety. Also the ethyl linker has been constrained providing information about the bioactive conformation of the amine functionality. However, combined 1,2-constriction by cyclization has only been tested with one compound. Here, we present three new 1,2-cyclized phenylethyl

SUBMITTER: Isberg V 

PROVIDER: S-EPMC3820707 | biostudies-literature | 2013

REPOSITORIES: biostudies-literature