Parallel synthesis and dopamine D(3)/D(2) receptor screening of novel {4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl}carboxamides.

Heidler P; Zohrabi Kalantari V; Calmels T; Capet M; Berrebi Bertrand I; Schwartz JC; Stark H; Link A

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Parallel synthesis and dopamine D(3)/D(2) receptor screening of novel {4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl}carboxamides.

机译：平行合成和新型{4-（4-（2-（2-甲氧基苯基）哌嗪-1-基）丁基}羧酰胺的多巴胺D（3）/ D（2）受体筛选。

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We have applied a fast and high-yielding method for the parallel amidation of 4-[4-(2-methoxyphenyl)piperazin-1-yl]-butylamine yielding analogs of the partial dopamine receptor agonist BP 897. Using this amino scaffold prepared in solution and polymer-bound carboxylic acid equivalents, we have synthesized a series of high affinity dopamine D(3) receptor ligands. The novel compounds were obtained in good to excellent yield and purity. Biological evaluation included determination of binding affinities at hD(2S) and hD(3) receptor subtypes. From the 22 novel structures presented here, compound 4v showed high affinity (K(i) (hD(3)) 1.6nM) and a 136-fold preference for the D(3) receptor versus that for the D(2) receptor subtype. Our results suggest that this derivatization technique is a useful method to speed up structure-activity relationships studies on dopamine receptor subtype modulators.

机译：我们已经对4- [4-（2-（2-甲氧基苯基）哌嗪-1-基]-丁胺进行平行酰胺化，并产生了部分多巴胺受体激动剂BP 897的类似物，采用了快速高效的方法。溶液和聚合物结合的羧酸当量，我们已经合成了一系列的高亲和力多巴胺D（3）受体配体。以良好至优异的产率和纯度获得了新型化合物。生物学评估包括确定hD（2S）和hD（3）受体亚型的结合亲和力。从此处介绍的22种新颖结构中，化合物4v显示出高亲和力（K（i）（hD（3））1.6nM），相对于D（2）受体亚型，D（3）受体具有136倍的偏好。我们的结果表明，这种衍生化技术是加快对多巴胺受体亚型调节剂的构效关系研究的有用方法。

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来源
《Bioorganic and Medicinal Chemistry》 |2005年第6期|P.2009-2014|共6页
作者
Heidler P; Zohrabi Kalantari V; Calmels T; Capet M; Berrebi Bertrand I; Schwartz JC; Stark H; Link A;
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作者单位

Institute of Pharmaceutical Chemistry, Philipps-University Marburg, Marbacher Weg 6, 35032 Marburg, Germany.;

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原文格式 PDF
正文语种 eng
中图分类基础医学;
关键词
receptor; novel; Dopamine; Aspects of disease screening; 多巴胺;

机译：受体;新颖;多巴胺;疾病筛查;多巴胺;

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Parallel synthesis and dopamine D(3)/D(2) receptor screening of novel {4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl}carboxamides.

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