当前位置： SCI文献检索 > Chemical Biology & Drug Design期刊下所有文献 > Solid-Supported Synthesis and 5-HT7 /5-HT1A Receptor Affinity of Arylpiperazinylbutyl Derivatives of 4,5-dihydro-1,2,4-triazine-6-(1H)-one.

Solid-Supported Synthesis and 5-HT7 /5-HT1A Receptor Affinity of Arylpiperazinylbutyl Derivatives of 4,5-dihydro-1,2,4-triazine-6-(1H)-one.

Abstract：

:A series of arylpiperazinylbutyl derivatives of 4,5-dihydro-1,2,4-triazine-6(1H)-ones was designed and synthesized according to the new solid-supported methodology. In this approach, triazinone scaffold was constructed from the Fmoc-protected glycine. The library representatives showed different levels of affinity for 5-HT7 and 5-HT1A receptors; compounds 13, 14 and 18-20 were classified as dual 5-HT7 /5-HT1A receptors ligands. The structure-affinity relationship analysis revealed that the receptor affinity and selectivity of the tested compounds depended on the kind of substituent in position 3 of triazinone fragment as well as substitution pattern of the phenylpiperazine moiety.

journal_name

Chem Biol Drug Des

journal_title

Chemical biology & drug design

authors

Grychowska K,Masurier N,Verdié P,Satała G,Bojarski AJ,Martinez J,Pawłowski M,Subra G,Zajdel P

doi

10.1111/cbdd.12539

subject

Has Abstract

pub_date

2015-10-01 00:00:00

pages

697-703

issue

4

eissn

1747-0277

issn

1747-0285

journal_volume

86

pub_type

杂志文章

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