| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10593122 | Bioorganic & Medicinal Chemistry Letters | 2012 | 4 Pages |
Abstract
A novel class of 4-alkoxy-[1â²-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4â²-piperidine)] analogues were designed and synthesized as H3R antagonists. Structure-activity relationship identified sulfone 27 with excellent H3R affinities in both humans and rats, and acceptable pharmacokinetic properties. Further, compound 28 achieved single digit nanomolar H3R affinities in both species with minimum hERG activity.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
![Synthesis and evaluation of 4-alkoxy-[1â²-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4â²-piperidine)] analogues as histamine-3 receptor antagonists](/preview/png/10593122.png "First Page Preview: Synthesis and evaluation of 4-alkoxy-[1â²-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4â²-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,