Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10587767 | Bioorganic & Medicinal Chemistry Letters | 2013 | 4 Pages |
Abstract
Potent small molecule antagonists of the urotensin receptor are described. These inhibitors were derived via systematically deconstructing a literature inhibitor to understand the basic pharmacophore and key molecular features required to inhibit the protein receptor. The series of benzylamine and benzylsulfone antagonists herein reported display a combination of nanomolar molecular and cellular potency as well as acceptable in vitro permeability and metabolic stability.
Related Topics
Physical Sciences and Engineering
Chemistry
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Authors
Steven J. Taylor, Fariba Soleymanzadeh, Ingo Muegge, Isamu Akiba, Naoyuki Taki, Saisoku Ueda, Elizabeth Mainolfi, Anne B. Eldrup,