AI Article Synopsis
- Researchers developed effective small molecule antagonists to block the urotensin receptor by analyzing existing inhibitors to identify essential molecular features.
- The new antagonists include benzylamine and benzylsulfone compounds that show strong potency at the nanomolar level for both molecular and cellular activities.
- These compounds also demonstrate good permeability and metabolic stability in laboratory tests, making them promising candidates for further study.
Article 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.
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| http://dx.doi.org/10.1016/j.bmcl.2013.01.105 | DOI Listing |
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