Referenced in: none

Automatically associated channels: Kv11.1

Title: Synthesis and evaluation of 4-alkoxy-[1'-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4'-piperidine)] analogues as histamine-3 receptor antagonists.

Authors: Nadine C Becknell, Reddeppa Reddy Dandu, Jacquelyn A Lyons, Lisa D Aimone, Rita Raddatz, Robert L Hudkins

Journal, date & volume: Bioorg. Med. Chem. Lett., 2012 Jan 1 , 22, 186-9

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/22153342

Abstract
A novel class of 4-alkoxy-[1'-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4'-piperidine)] analogues were designed and synthesized as H(3)R antagonists. Structure-activity relationship identified sulfone 27 with excellent H(3)R affinities in both humans and rats, and acceptable pharmacokinetic properties. Further, compound 28 achieved single digit nanomolar H(3)R affinities in both species with minimum hERG activity.