Synthesis of some tricyclic heteroaromatic systems and their A1 and A2a adenosine binding activity
摘要:
The syntheses, A(1) and A(2a) adenosine receptor affinities and structure-activity relationships of some 2-aryl-1,2,4-triazolo[1,5-a]quinoxalines, 2-arylimidazo[1,2-a]quinoxalines, 1-arylimidazo[1,5-a]quinoxalines are reported and compared with that of a previously reported 2-phenylpyrazolo[1,5-a]quinoxaline. The results show that some triazoloquinoxalines are potent and specific A(1) adenosine receptor ligands and that the replacement of either nitrogen at position 1 or 3 of the triazoloquinoxaline moiety with a CH brought about a decrease in affinity at both adenosine receptors.
IMIDAZOL[1,2-alpha]QUINOXALINES AND DERIVATIVES FOR THE TREATMENT OF CANCERS
申请人:Deleuze-Masquefa Carine
公开号:US20100249142A1
公开(公告)日:2010-09-30
Imidazo[1,2-a]quinoxaline compounds for the treatment of cancers as well as pharmaceutical compositions that include these compounds and their uses in therapy.
The compound of general formula (I):
The syntheses, A(1) and A(2a) adenosine receptor affinities and structure-activity relationships of some 2-aryl-1,2,4-triazolo[1,5-a]quinoxalines, 2-arylimidazo[1,2-a]quinoxalines, 1-arylimidazo[1,5-a]quinoxalines are reported and compared with that of a previously reported 2-phenylpyrazolo[1,5-a]quinoxaline. The results show that some triazoloquinoxalines are potent and specific A(1) adenosine receptor ligands and that the replacement of either nitrogen at position 1 or 3 of the triazoloquinoxaline moiety with a CH brought about a decrease in affinity at both adenosine receptors.