Please use this identifier to cite or link to this item: http://www.repositorio.ufop.br/handle/123456789/5121
Title: Prostaglandin E2-bisphosphonate conjugates : potential agents for treatment of osteoporosis.
Authors: Gil, Laurent Frédéric
Han, Yongxin
Opas, Evan E.
Rodan, Gideon A.
Ruel, Réjean
Keywords: Osteoporosis
Prostaglandin E2
Bisphosphonate
Alendronate
Conjugate
Issue Date: 1999
Citation: GIL, L. F. et al. Prostaglandin E2-bisphosphonate conjugates: potential agents for treatment of osteoporosis. Bioorganic & Medicinal Chemistry, v. 7, p. 901-919, 1999. Disponível em: <http://www.sciencedirect.com/science/article/pii/S0968089699000450>. Acesso em: 02 fev. 2015.
Abstract: Conjugates of bisphosphonates (potential bone resorption inhibitors) and prostaglandin E2 (a bone formation enhancer) were prepared and evaluated for their ability to bind to bone and to liberate, enzymatically, free PGE2. The conjugate 3, an amide at C-1 of PGE2 proved to be too stable in vivo while conjugate 6, a thioester, was too labile. Several PGE2, C-15 ester-linked con- jugates (18, 23, 24 and 31) were prepared and conjugate 23 was found to bind effectively to bone in vitro and in vivo and to liberate PGE2 at an acceptable rate. A 4-week study in a rat model of osteoporosis showed that 23 was better tolerated and more effective as a bone growth stimulant than daily maximum tolerated doses of free PGE2.
URI: http://www.repositorio.ufop.br/handle/123456789/5121
metadata.dc.identifier.doi: https://doi.org/10.1016/S0968-0896(99)00045-0
ISSN: 0968-0896
metadata.dc.rights.license: O periódico Bioorganic & Medicinal Chemistry concede permissão para depósito deste artigo no Repositório Institucional da UFOP. Número da licença: 3581981508139.
Appears in Collections:DEQUI - Artigos publicados em periódicos

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