17879-89-9Relevant academic research and scientific papers
Specific enzyme inhibitors in vitamin biosynthesis. Part 3. The synthesis and inhibitory properties of some substrates and transition state analogues of riboflavin synthase
Al-Hassan, Saieba S.,Kulick, Russell J.,Livingstone, Daniel B.,Suckling, Colin J.,Wood, Hamish C. S.,Wrigglesworth, Roger,Ferone, Robert
, p. 2645 - 2656 (2007/10/02)
Syntheses of potential inhibitors of riboflavin synthase are described. The tolerance of the enzyme to bulky substituents was investigated by the synthesis of substrate analogues which included lumazines and pyrido[2,3-d]-pyrimidines prepared by condensation of α-diketones and β-keto-aldehydes respectively with appropriate amino-substituted uracils. Potential transition-state analogues, including 7-oxolumazines, 7-oxopyrido[2,3-d] pyrimidines, and 6,7-dioxolumazines were also prepared by similar condensations using α-keto-acid derivatives, dimethyl acetylenedicarboxylate, and oxalate derivatives. Two possible dual affinity inhibitors were also prepared. The potential inhibitors were tested using riboflavin synthase from yeast or from E. coli, and their effectiveness is discussed in relation to the bulk and electronic character of the substituents.
Trioxopteridine derivatives suitable as medicament
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, (2008/06/13)
Trioxopteridine derivatives of the formula STR1 , wherein R1 is a normal alkyl group having 0 to 6 hydroxyl groups and R2 is hydrogen or a normal lower alkyl group having 0 to 5 hydroxyl groups, are prepared by catalytically hydrogenating a 6-substituted-5-nitro-2,4-dioxopyrimidine to give a 6-substituted-5-amino-2,4-dioxopyrimidine, and then reacting the latter compound with a compound of the formula R2 --A--COOR3, wherein R3 is hydrogen, lower alkyl, an alkali metal or an alkaline earth metal and A is carbonyl or a group of the formula STR2 wherein R4 is lower alkyl. The resulting trioxopteridine derivatives have analgesic and antiphlogistic properties and are therefore useful as pharmaceutical medicaments.
6-L-dihydroxyethyl-2,4,7-trioxo-8-D-ribityl pteridine and process for producing the same
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, (2008/06/13)
Trioxopteridine derivatives of the formula SPC1 , wherein R1 is a normal alkyl group having 0 to 6 hydroxyl groups and R2 is hydrogen or a normal lower alkyl group having 0 to 5 hydroxyl groups, are prepared by catalytically hydrogenating a 6-substituted-5-nitro-2,4-dioxopyrimidine to give a 6-substituted-5-amino-2,4-dioxopyrimidine, and then reacting the latter compound with a compound of the formula R2 --A--COOR3, wherein R3 is hydrogen, lower alkyl, an alkali metal or an alkaline earth metal and A is carbonyl or a group of the formula EQU1 wherein R4 is lower alkyl. The resulting trioxopteridine derivatives have analgesic and antiphlogistic properties and are therefore useful as pharmaceutical medicaments.
