Talipexole variations as novel bitopic dopamine D2 and D3 receptor ligands,RSC Medicinal Chemistry

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Talipexole variations as novel bitopic dopamine D2 and D3 receptor ligands
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2019-08-27 , DOI: 10.1039/c9md00379g
Lars Stank _{1,

2,

3,

4} , Annika Frank _{1,

2,

3,

4} , Stefanie Hagenow _{1,

2,

3,

4} , Holger Stark _{1,

2,

3,

4}

Affiliation

We linked 2-aminothiazoloazepane scaffolds with phenylpiperazine pharmacophores to generate bitopic dopamine receptor ligands. Highest D₂R/D₃R binding affinities up to pK_i values of 7.74 were observed for compounds containing a 1-(2,3-dichlorophenyl)piperazinoyl moiety, maintaining affinity with deaminated 5,6,7,8-tetrahydro-4H-thiazoloazepine derivatives.

中文翻译：

Talipexole变异作为新型的双向多巴胺D2和D3受体配体

我们将2-aminothiazoloazepane支架与苯基哌嗪药效团连接在一起，以生成双位多巴胺受体配体。对于含有1-（2,3-二氯苯基）哌嗪酰基的化合物，与去氨基的5,6,7,8-四氢-羟基化合物保持亲和力，观察到的最高D ₂ R / D ₃ R结合亲和力高达p K _i值为7.74。 4 H-噻唑并ze庚因衍生物。

更新日期：2019-08-27

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