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.
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Authors | W 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 |
Journal | Bioorganic & medicinal chemistry letters
(Bioorg Med Chem Lett)
Vol. 9
Issue 13
Pg. 1807-12
(Jul 05 1999)
ISSN: 0960-894X [Print] England |
PMID | 10406646
(Publication Type: Journal Article)
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Chemical References |
- Acetates
- Aminopyridines
- Benzodiazepinones
- Receptors, Vitronectin
- SB 223245
- SB 265123
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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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