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Orally bioavailable nonpeptide vitronectin receptor antagonists with efficacy in an osteoporosis model.

Abstract
A new series of potent nonpeptide vitronectin receptor antagonists, based on a novel carbocyclic Gly-Asp mimetic, has been discovered. A representative of this series, SB 265123 (4), has 100% oral bioavailability in rats, and is orally active in vivo in the ovariectomized rat model of osteoporosis.
AuthorsW H Miller, W E Bondinell, R D Cousins, K F Erhard, D R Jakas, R M Keenan, T W Ku, K A Newlander, S T Ross, R C Haltiwanger, J Bradbeer, F H Drake, M Gowen, S J Hoffman, S M Hwang, I E James, M W Lark, B Lechowska, D J Rieman, G B Stroup, J A Vasko-Moser, D L Zembryki, L M Azzarano, P C Adams, W F Huffman
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 9 Issue 13 Pg. 1807-12 (Jul 05 1999) ISSN: 0960-894X [Print] England
PMID10406646 (Publication Type: Journal Article)
Chemical References
  • Acetates
  • Aminopyridines
  • Benzodiazepinones
  • Receptors, Vitronectin
  • SB 223245
  • SB 265123
Topics
  • Acetates (chemical synthesis, pharmacokinetics)
  • Administration, Oral
  • Aminopyridines (chemical synthesis, pharmacokinetics)
  • Animals
  • Benzodiazepinones (chemical synthesis, pharmacokinetics)
  • Biological Availability
  • Disease Models, Animal
  • Kinetics
  • Osteoporosis (drug therapy)
  • Rats
  • Receptors, Vitronectin (antagonists & inhibitors)
  • Time Factors

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