
Chemical and Pharmaceutical Bulletin p. 245 - 248 (1992)
Update date:2022-08-06
Topics:
Miyahara
Kasugai
Ohmomo
Tanaka
Tanimoto
Various analogues of benzyl 5-phenyl-2-oxazolecarbamate (1a) were synthesized, and the structure-activity relationship of these analogues as aldose reductase inhibitor was studied. The carbamate group was necessary for the inhibitory activity. The introduction of an alkyl group at the C-4 position of 1a enhanced the inhibitory activity, however, the N-carboxymethyl group on the carbamate moiety counteracted to a hydrophobic interaction between the alkyl group at the C-4 position and the enzyme molecule.
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