Model studies on a synthetically facile series of N-substituted phenyl-N'-pyridin-3-yl ureas leading to 1-(3-pyridylcarbamoyl) indolines that are potent and selective 5-HT(2C/2B) receptor antagonists.

Abstract A model series of 5-HT 2C antagonists have been prepared by rapid parallel synthesis. These N -substituted phenyl- N ′-pyridin-3-yl ureas were found to have a range of 5-HT 2C receptor affinities and selectivities over the closely related 5-HT 2A receptor. Extrapolation of simple SAR, derived from this set of compounds, to the more active but synthetically more complex 1-(3-pyridyl-carbamoyl)indoline series allowed us to target optimal substitution patterns and identify potent and selective 5-HT 2C/2B antagonists.