128043-67-4Relevant academic research and scientific papers
Structure-activity relationship of 2,4,5-trioxoimidazolidines as inhibitors of thymidine phosphorylase
Rajabi, Mehdi,Mansell, David,Freeman, Sally,Bryce, Richard A.
, p. 1165 - 1171 (2011/04/17)
Novel non-nucleobase-derived inhibitors of the angiogenic enzyme, thymidine phosphorylase, have been identified using molecular modelling, synthesis and biological evaluation. These inhibitors are 2,4,5-trioxoimidazolidines bearing N-(substituted)phenylalkyl groups, together with, in most cases, N′-(CH2)n-carboxylic acid, ester or amide side chains. The best compound from this series is 3-(2,4,5-trioxo-3-phenylethyl- imidazolodin-1-yl)propionamide, with an IC50 of 40 μM against Escherichia coli TP. Molecular modelling suggests that this ligand, when complexed with closed-cleft human TP, would have the phenylalkyl group in the active site region normally occupied by a thymine-containing structure.
Highly selective aldose reductase inhibitors. 1. 3-(Arylalkyl)-2,4,5- trioxoimidazolidine-1-acetic acids
Ishii,Kotani,Nagaki,Shibayama,Toyomaki,Okukado,Ienaga,Okamoto
, p. 1924 - 1927 (2007/10/03)
A series of 3-(arylalkyl)-2,4,5-trioxoimidazolidine-1-acetic acids (1) was prepared and tested for aldose reductase (AR) and aldehyde reductase (ALR) inhibitory activities. These compounds showed strong inhibitory activity against AR without significant inhibitory activity for ALR. The ratio of IC50(ALR)IC50(AR) was > 1000 in some compounds. On the basis of pharmacological tests such as the recovery of reduced motor nerve conduction velocity and toxicological profile, 3-(3-nitrobenzyl)-2,4,5- trioxoimidazolidine-1-acetic acid (NZ-314) was selected as the candidate for clinical development.
PARABANIC ACID DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF
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, (2008/06/13)
Parabanic acid compound of the formula (I): wherein R is hydrogen or a lower alkyl group, X is hydrogen, an alkyl group, a cycloalkyl group, a lower alkylcycloalkyl group, a phenyl group or a phenalkyl group, and n represents an integer of 1 to 4, exhibit
