11495581 |
Mylari BL, Oates PJ, Beebe DA, Brackett NS, Coutcher JB, Dina MS, Zembrowski WJ: Sorbitol dehydrogenase inhibitors (SDIs): a new potent, enantiomeric SDI, 4-[2-1R-hydroxy-ethyl)-pyrimidin-4-yl] piperazine-1-sulfonic acid dimethylamide. J Med Chem. 2001 Aug 16;44(17):2695-700.
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32(0,1,1,2) |
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11784155 |
Chu-Moyer MY, Ballinger WE, Beebe DA, Berger R, Coutcher JB, Day WW, Li J, Mylari BL, Oates PJ, Weekly RM: Orally-effective, long-acting sorbitol dehydrogenase inhibitors: synthesis, structure-activity relationships, and in vivo evaluations of novel heterocycle-substituted piperazino-pyrimidines. J Med Chem. 2002 Jan 17;45(2):511-28.
However, the desired in vivo potency in chronically diabetic rats, ED (90) < or = 5 mg/kg/day, was achieved only through further modification of the piperazine linker. |
3(0,0,0,3) |
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