Phenylsulfonylnitromethanes as potent irreversible inhibitors of aldose reductase
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...
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Published in | European journal of medicinal chemistry Vol. 34; no. 9; pp. 745 - 751 |
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Main Authors | , , , , |
Format | Journal Article |
Language | English |
Published |
ISSY-LES-MOULINEAUX
Elsevier Masson SAS
01.09.1999
Elsevier |
Subjects | |
Online Access | Get full text |
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Summary: | 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 IC
50s between 0.01 and 0.19 μM. Some of the compounds are also potent affinity labels for AR. Compound
19 exhibits the highest and almost complete irreversible inhibition of AR known to date. |
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ISSN: | 0223-5234 1768-3254 |
DOI: | 10.1016/S0223-5234(99)00219-6 |