105686-05-3Relevant articles and documents
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.
Pharmaceutical composition containing an imidazolidinetrione derivative or pharmaceutically acceptable salt thereof
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, (2008/06/13)
Pharmaceutical compositions containing imidazolidinetrione derivatives or pharmaceutically acceptable salts thereof having hypoglycemic and hypolipidemic effects. The compositions comprise as an active ingredient at least one imidazolidinetrione derivative of the formula: STR1 wherein each of R1 and R2, which may be the same or different, is hydrogen, an alkyl group, a cycloalkyl group or STR2 and each of R3 and R4, which may be the same or different, is hydrogen, halogen, a nitro group, a lower alkyl group or a lower alkoxy group.
