Phenylsulfonylnitromethanes as potent irreversible inhibitors of aldose reductase

NH Saab, IO Donkor, L Rodriguez, PF Kador…

Index: Saab, Nada H.; Donkor, Isaac O.; Rodriguez, Libaniel; Kador, Peter F.; Miller, Duane D. European Journal of Medicinal Chemistry, 1999 , vol. 34, # 9 p. 745 - 751

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Citation Number: 10

Abstract

Aldose reductase (AR) inhibition provides a viable pharmacologically direct mode for the treatment of diabetic complications. We have synthesized a series of N-4 substituted analogues (15–21) of the known aldose reductase inhibitor phenyl-sulfonylnitromethane. The compounds are potent inhibitors of AR with IC50s between 0.01 and 0.19 μM. Some of the compounds are also potent affinity labels for AR. Compound 19 exhibits the highest ...