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J Med Chem. 2003 Jun 5;46(12):2283-6.

A highly selective, non-hydantoin, non-carboxylic acid inhibitor of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran- 2-sulfonyl)-2-H-pyridazin-3-one.

Author information

1
Pfizer Global Research and Development, Pfizer Inc., Groton, Connecticut 06340, USA. blmylari@aol.com

Abstract

We report here on the discovery path that led to a structurally unprecedented non-hydantoin, non-carboxylic acid aldose reductase inhibitor, 24, which shows remarkably potent oral activity in normalizing elevated sorbitol levels and, more significantly, fructose levels in the sciatic nerve of chronically diabetic rats, with ED(90) values of 0.8 and 3 mpk, respectively. It is well absorbed in rats (oral bioavailability, 98%) and has a long plasma t(1/2) (26 +/- 3 h).

PMID:
12773033
DOI:
10.1021/jm034065z
[Indexed for MEDLINE]

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