Highly potent geminal bisphosphonates. From pamidronate disodium (Aredia) to zoledronic acid (Zometa)

…, J Schmid, G Schreiber, Y Seltenmeyer…

文献索引：Widler, Leo; Jaeggi, Knut A.; Glatt, Markus; Mueller, Klaus; Bachmann, Rolf; Bisping, Michael; Born, Anne-Ruth; Cortesi, Reto; Guiglia, Gabriela; Jeker, Heidi; Klein, Remy; Ramseier, Ueli; Schmid, Johann; Schreiber, Gerard; Seltenmeyer, Yves; Green, Jonathan R. Journal of Medicinal Chemistry, 2002 , vol. 45, # 17 p. 3721 - 3738

全文：HTML全文

被引用次数: 284

摘要

Bisphosphonates (BPs) are pyrophosphate analogues in which the oxygen in POP has been replaced by a carbon, resulting in a metabolically stable PCP structure. Pamidronate (1b, Novartis), a second-generation BP, was the starting point for extensive SAR studies. Small changes of the structure of pamidronate lead to marked improvements of the inhibition of osteoclastic resorption potency. Alendronate (1c, MSD), with an extra methylene group ...