13-10173. Zenarestat [Archived]

Nomenclature

CAS number: 112733-06-9
3-[(4-Bromo-2-fluorophenyl)methyl]-7-chloro-3,4-dihydro-2,4-dioxo-1(2H)-quinazolineacetic acid; 3-(4-bromo-2-fluorobenzyl)-7-chloro-2,4-dioxo-1,2,3,4-tetrahydroquinazoline-1-acetic acid; FK-366; FR-74366.
C17H11BrClFN2O4; mol wt 441.64.
C 46.23%, H 2.51%, Br 18.09%, Cl 8.03%, F 4.30%, N 6.34%, O 14.49%.

Description and references

Aldose reductase inhibitor. Prepn: M. Hashimoto et al., EP 218999; eidem, US 4734419 (1987, 1988 both to Fujisawa). Inhibition kinetics and effect on sorbitol accumulation: S. Ao et al., Metabolism 40, 77 (1991). Pharmacokinetics and metabolism in diabetic rats: Y. Tanaka et al., Drug Metab. Dispos. 21, 677 (1993). Clinical pharmacology: M. Kanamaru et al., J. Clin. Pharmacol. 33, 1122 (1993).

Chemical structure

Properties

Crystals from ethanol + water, mp 223-224°.

Therapeutic Category

In treatment of diabetic neuropathy and cataract.

Keywords

Aldose Reductase Inhibitor

Status

This monograph has been retired and is no longer subject to revision or update.