Solid-Supported Synthesis and 5-HT 7 /5-HT 1A Receptor Affinity of Arylpiperazinylbutyl Derivatives of 4,5-dihydro-1,2,4-triazine-6-(1 H )-one - CNRS - Centre national de la recherche scientifique Accéder directement au contenu
Article Dans Une Revue Chemical Biology and Drug Design Année : 2015

Solid-Supported Synthesis and 5-HT 7 /5-HT 1A Receptor Affinity of Arylpiperazinylbutyl Derivatives of 4,5-dihydro-1,2,4-triazine-6-(1 H )-one

Résumé

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.

Domaines

Chimie

Dates et versions

hal-03564059 , version 1 (10-02-2022)

Identifiants

Citer

Katarzyna Grychowska, Nicolas Masurier, Pascal Verdié, Grzegorz Satała, Andrzej Bojarski, et al.. Solid-Supported Synthesis and 5-HT 7 /5-HT 1A Receptor Affinity of Arylpiperazinylbutyl Derivatives of 4,5-dihydro-1,2,4-triazine-6-(1 H )-one. Chemical Biology and Drug Design, 2015, 86 (4), pp.697-703. ⟨10.1111/cbdd.12539⟩. ⟨hal-03564059⟩
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