Inhibition of aldose reductases from rabbit lens by oxazole derivatives.
- 1 January 1984
- journal article
- research article
- Published by Pharmaceutical Society of Japan in CHEMICAL & PHARMACEUTICAL BULLETIN
- Vol. 32 (3) , 1032-1039
- https://doi.org/10.1248/cpb.32.1032
Abstract
Twenty kinds of oxazole derivatives having various substituents at the C-2 and C-5 positions were synthesized and tested in vitro for inhibition of rabbit lens aldose reductase (Ia and Ib), the enzyme that initiates cataract formation in diabetes. Compounds possessing bulky groups at C-2 and C-5 of the oxazole skeleton were found to be potent inhibitors. Benzyl 5-phenyl-2-oxazolecarbamate (12) inhibited aldose reductases Ia and Ib by 50% at about 15μM. N-Phenyl-N'-(5-phenyl-2-oxazolyl) urea also exhibited inhibitory activity comparable to that of compound 12. The structure-inhibitory activity relationships are discussed.Keywords
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