Deconstruction of sulfonamide inhibitors of the urotensin receptor (UT) and design and synthesis of benzylamine and benzylsulfone antagonists.
| Autor: | Taylor SJ; Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Rd., PO Box 368, Ridgefield, CT 06877-036, USA. steven.taylor@boehringer-ingelheim.com, Soleymanzadeh F, Muegge I, Akiba I, Taki N, Ueda S, Mainolfi E, Eldrup AB |
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| Jazyk: | angličtina |
| Zdroj: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2013 Apr 01; Vol. 23 (7), pp. 2177-80. Date of Electronic Publication: 2013 Feb 04. |
| DOI: | 10.1016/j.bmcl.2013.01.105 |
| Abstrakt: | 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. (Copyright © 2013 Elsevier Ltd. All rights reserved.) |
| Databáze: | MEDLINE |
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