Synthesis and evaluation as NOP ligands of some spiro[piperidine-4,2′(1′H)-quinazolin]-4′(3′H)-ones and spiro[piperidine-4,5′(6′H)[1,2,4]triazolo[1,5-c]quinazolines]

Synthesis and evaluation as NOP ligands of some spiro[piperidine-4,2′(1′H)-quinazolin]-4′(3′H)-ones and spiro[piperidine-4,5′(6′H)[1,2,4]triazolo[1,5-c]quinazolines]
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DOI:
10.1248/cpb.54.611
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发表时间:
2006-05-01
影响因子:
1.7
通讯作者:
Del Giudice, Maria Rosaria
Del Giudice, Maria Rosaria
中科院分区:
医学4区
文献类型:
--
作者:
Mustazza, Carlo;Borioni, Anna;Del Giudice, Maria Rosaria

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合成了一些螺[哌啶-4,2 '(1' H)-喹唑啉]-4 '(3' H)-酮3和螺[哌啶-4,5 '(6' H)-[1,2,4]三唑并[1,5-c]喹唑啉] 4,并评价了它们作为痛敏素受体的配体。所检测的化合物显示部分激动活性,除了化合物3,4 n被证明是纯拮抗剂。
Some spiro[piperidine-4,2'(1'H)-quinazolin]-4'(3'H)-ones 3 and spiro[piperidine-4,5'(6'H)-[1,2,4]triazolo[1,5-c]quinazolines] 4 were synthesized and evaluated as ligands of the nociceptin receptor. The examined compounds showed partial agonistic activity, except compounds 3,4n that proved to be pure antagonists.