Abstract:
:In order to elucidate the key atoms and/or stereostructures necessary for the inhibitory emergence of aldose reductase, crystal structure determinations were carried out for 11 oxazolecarbamate analogues, which have similar chemical and physicochemical properties but different inhibitory activities. The molecular conformations, revealed by X-ray analyses, were also ascertained to be energetically stable from theoretical conformational energy calculations. A surprising degree of conformational similarity was observed for the potent inhibitors. The analyses of the quantitative structure--activity relationships showed that the molecular conformation and the dipole moment, as well as the hydrophobicity at the oxazole C5-site, were important for high activity.
journal_name
Mol Pharmacoljournal_title
Molecular pharmacologyauthors
Ishida T,In Y,Ohishi H,Yamamoto D,Inoue M,Tanaka C,Ueno Y,Ohmomo Y,Kanda N,Tanaka Asubject
Has Abstract,Author List Incompletepub_date
1988-09-01 00:00:00pages
377-87issue
3eissn
0026-895Xissn
1521-0111journal_volume
34pub_type
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