2. Academic Validation
  3. Deconstruction of sulfonamide inhibitors of the urotensin receptor (UT) and design and synthesis of benzylamine and benzylsulfone antagonists

Deconstruction of sulfonamide inhibitors of the urotensin receptor (UT) and design and synthesis of benzylamine and benzylsulfone antagonists

  • Bioorg Med Chem Lett. 2013 Apr 1;23(7):2177-80. doi: 10.1016/j.bmcl.2013.01.105.
Steven J Taylor 1,  Fariba Soleymanzadeh,  Ingo Muegge,  Isamu Akiba,  Naoyuki Taki,  Saisoku Ueda,  Elizabeth Mainolfi,  Anne B Eldrup
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Rd., PO Box 368, Ridgefield, CT 06877-036, USA. steven.taylor@boehringer-ingelheim.com
PMID: 23453841 DOI: 10.1016/j.bmcl.2013.01.105
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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