| Autor: |
Duggan ME; Departments of Medicinal Chemistry, Bone Biology and Osteoporosis Research, and Pharmacology, Merck Research Laboratories, West Point, Pennsylvania 19486, USA., Duong LT, Fisher JE, Hamill TG, Hoffman WF, Huff JR, Ihle NC, Leu CT, Nagy RM, Perkins JJ, Rodan SB, Wesolowski G, Whitman DB, Zartman AE, Rodan GA, Hartman GD |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 2000 Oct 05; Vol. 43 (20), pp. 3736-45. |
| DOI: |
10.1021/jm000133v |
| Abstrakt: |
Modification of the potent fibrinogen receptor (alpha(IIb)beta(3)) antagonist 1 generated compounds with high affinity for the vitronectin receptor alpha(v)beta(3). Sequential modification of the basic N-terminus of 1 led to the identification of the 5,6,7, 8-tetrahydro[1,8]naphthyridine moiety (THN) as a lipophilic, moderately basic N-terminus that provides molecules with excellent potency and selectivity for the integrin receptor alpha(v)beta(3). The THN-containing analogue 5 is a potent inhibitor of bone resorption in vitro and in vivo. In addition, the identification of a novel, nonpeptide radioligand with high affinity to alpha(v)beta(3) is also reported. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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