6943-94-8Relevant academic research and scientific papers
3,5-dioxo-(2H,4H)-1,2,4-triazine derivatives as 5HT1A ligands
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, (2008/06/13)
A 3,5-dioxo-(2H,4H)-1,2,4-triazine compounds of formula I STR1 in which: R1 and R2, which are identical or different, represent hydrogen or C1 -C6 alkyl, n is 2 to 6, inclusive, A represents aryl piperazino II STR2 the Ar grouping representing phenyl, naphthyl, pyrimidyl, or pyridyl, unsubstituted or substituted by C1 -C3 alkyl, C1 -C3 alkoxy, hydroxy, trifluoromethyl, or halogen, or III benzodioxanyl-methyl-amino or pyridodioxanyl-methyl-amino STR3 in which R represents hydrogen or C1 -C3 alkyl and X represents a nitrogen or carbon atom, therapeutically-acceptable salts and enantiomers thereof, pharmaceutical compositions thereof, and method for treatment of diseases requiring a 5HT1A receptor agonist therewith.
Anticoccidial derivatives of 6 azauracil. I. Enhancement of activity by benzylation of nitrogen 1. Observations on the design of nucleotide analogues in chemotherapy
Mylari,Miller,Howes Jr.,Figdor,Lynch,Koch
, p. 475 - 483 (2007/10/09)
Benzylation of 6-azauracil at N-1 (which corresponds to the point of attachment of the ribose phosphate unit in pyrimidine nucleotides) has been found to augment its anticoccidial activity fourfold. The high potency of 1-benzyl-6-azauracil is ascribed to a combination of intrinsic activity, efficient oral absorption, and a moderate rate of excretion. Metabolism experiments using 1-benzyl-6-azauracil labeled with 14C in the heterocycle and (separately) in the side chain showed that, in the drug accounted for, no cleavage had occurred. Additional activity increases were achieved by introducing small, electron-withdrawing substituents in the meta and/or para position(s) of the benzyl group. One of the most active derivatives, 1-(3-cyanobenzyl)-6-azauracil, is about 16 times as potent as 6-azauracil.
