Benzoxazoline and benzimidazoline derivatives as novel aldose reductase inhibitors, part 2: Lead optimization

Authors
Nakao, K Asao, M Shirai, H Saito, K Moriya, T Iwata, H Matsumoto, M Matsuoka, Y Shimizu, R
Citation
K. Nakao et al., Benzoxazoline and benzimidazoline derivatives as novel aldose reductase inhibitors, part 2: Lead optimization, MED CHEM RE, 9(7-8), 1999, pp. 631-642
Citations number
11
Categorie Soggetti
Chemistry & Analysis
Journal title
MEDICINAL CHEMISTRY RESEARCH
ISSN journal
10542523 → ACNP
Volume
9
Issue
7-8
Year of publication
1999
Pages
631 - 642
Database
ISI
SICI code
1054-2523(1999)9:7-8<631:BABDAN>2.0.ZU;2-L
Abstract
We designed novel aldose reductase inhibitors, benzoxazoline and benzimidaz oline derivatives, bas ed on lead evolution from spiroquinazolinones. In or der to optimize in vivo activity in the lens, variously substituted derivat ives were synthesized. The relationship between structure and in vitro acti vity was also analyzed by comparative molecular field analysis. The optimiz ed compound exhibited high potency in the lens.