A Sorbitol Dehydrogenase Inhibitor of Exceptional in Vivo Potency with a Long Duration of Action: 1-(R)-{4-[4-(4,6-Dimethyl[1,3,5]triazin-2-yl)- 2R,6S-dimethylpiperazin-1-yl]pyrimidin-2- yl}ethanol
Journal of Medicinal Chemistry2002Vol. 45(20), pp. 4398–4401
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Banavara L. Mylari, Peter J. Oates, William J. Zembrowski, David A. Beebe, Edward L. Conn, James B. Coutcher, Melissa O’Gorman, Michael C. Linhares, Gregory J. Withbroe
Abstract
We report here a novel sorbitol dehydrogenase inhibitor, 16, that shows very high oral potency (50 microg/kg) in normalizing elevated fructose levels in the sciatic nerve of chronically diabetic rats and sustained duration of action (>24 h). Furthermore, 16 shows attractive pharmaceutical properties, including good solubility in simulated human gastric fluid, excellent Caco-2 Papp, moderate lipophilicity, and metabolic stability for achieving good oral absorption and long duration of action.
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