2. Academic Validation
  3. The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists

The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists

  • Bioorg Med Chem Lett. 2009 Aug 15;19(16):4740-2. doi: 10.1016/j.bmcl.2009.06.057.
Ian M Bell 1,  Rodney A Bednar,  Halea A Corcoran,  John F Fay,  Steven N Gallicchio,  Victor K Johnston,  James C Hershey,  Cynthia M Miller-Stein,  Eric L Moore,  Scott D Mosser,  Shane A Roller,  Christopher A Salvatore,  Cory R Theberge,  Bradley K Wong,  C Blair Zartman,  Stefanie A Kane,  Theresa M Williams,  Samuel L Graham,  Joseph P Vacca
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. ian_bell@merck.com
PMID: 19577468 DOI: 10.1016/j.bmcl.2009.06.057
Abstract

A series of tricyclic CGRP Receptor antagonists was optimized in order to improve oral bioavailability. Attenuation of polar surface area and incorporation of a weakly basic indoline nitrogen led to compound 5, a potent antagonist with good oral bioavailability in three species.

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