SYNTHESIS OF SOME TRICYCLIC HETEROAROMATIC SYSTEMS AND THEIR A(1) AND A(2A) ADENOSINE BINDING-ACTIVITY

SYNTHESIS OF SOME TRICYCLIC HETEROAROMATIC SYSTEMS AND THEIR A(1) AND A(2A) ADENOSINE BINDING-ACTIVITY
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DOI:
10.1016/0223-5234(96)88218-3
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发表时间:
1995-01-01
影响因子:
6.7
通讯作者:
LUCACCHINI, A
LUCACCHINI, A
中科院分区:
医学1区
文献类型:
--
作者:
COLOTTA, V;CECCHI, L;LUCACCHINI, A

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报道了2-芳基-1,2,4-三唑并[1,5-a]喹喔啉、2-芳基咪唑并[1,2-a]喹喔啉、1-芳基咪唑并[1,5-a]喹喔啉的合成、A(1)和A(2a)腺苷受体亲和力及构效关系,并与文献报道的2-苯基吡唑并[1,5-a]喹喔啉进行了比较。结果表明,一些三唑喹喔啉是有效的和特异性的A(1)腺苷受体配体,并且用CH取代三唑喹喔啉部分的1位或3位的氮导致对两种腺苷受体的亲和力降低。
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.