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ID: ALA1134237
Journal: Bioorg Med Chem Lett
Title: Discovery of zoniporide: a potent and selective sodium-hydrogen exchanger type 1 (NHE-1) inhibitor with high aqueous solubility.
Authors: Guzman-Perez A, Wester RT, Allen MC, Brown JA, Buchholz AR, Cook ER, Day WW, Hamanaka ES, Kennedy SP, Knight DR, Kowalczyk PJ, Marala RB, Mularski CJ, Novomisle WA, Ruggeri RB, Tracey WR, Hill RJ.
Abstract: Zoniporide (CP-597,396) is a potent and selective inhibitor of NHE-1, which exhibits high aqueous solubility and acceptable pharmacokinetics for intravenous administration. The discovery, synthesis, activities, and rat and dog pharmacokinetics of this compound are presented. The potency and selectivity of zoniporide may be due to the conformation that the molecule adopts due to the presence of a cyclopropyl and a 5-quinolinyl substituent on the central pyrazole ring of the molecule.
CiteXplore: 11277524