877867-16-8Relevant academic research and scientific papers
Non-basic ligands for aminergic GPCRs: The discovery and development diaryl sulfones as selective, orally bioavailable 5-HT2A receptor antagonists for the treatment of sleep disorders
Ladduwahetty, Tammy,Gilligan, Myra,Humphries, Alexander,Merchant, Kevin J.,Fish, Rebecca,McAlister, George,Ivarsson, Magnus,Dominguez, Maria,O'Connor, Desmond,MacLeod, Angus M.
scheme or table, p. 3708 - 3712 (2010/09/18)
Scaffold hopping from a non-basic series of 5-HT2A receptor antagonists developed in-house that possessed reduced activity in vivo enabled the discovery of a novel series of diaryl sulfones that gave excellent occupancy on oral dosing. Not only does this work further demonstrate that oral bioavailability of a given series can be enhanced by improving physicochemical parameters such as log P, but it corroborates the growing evidence that a protonated amine is not essential for affinity at aminergic GPCRs.
DIARYLSULFONES AS 5-HT2A ANTAGONISTS
-
Page/Page column 43, (2008/06/13)
Compounds of formula (I) are potent and selective antagonists of the human 5-HT2A receptor, and hence useful in treatment of a variety of adverse conditions of the CNS.
