色胺
化学
受体
对接(动物)
同源建模
立体化学
5-羟色胺受体
胺气处理
生物化学
血清素
组合化学
色胺
酶
医学
有机化学
护理部
作者
Amir Hanna-Elias,David T. Manallack,Isabelle Berque‐Bestel,Helen Irving,Ian M Coupar,Magdy N. Iskander
标识
DOI:10.2174/092986710791859351
摘要
For the development of novel 5-HT4 receptor ligands we have designed and synthesized two series of 5- methoxytryptamine derivatives varying the substitution on the primary amine. Their biological activities were evaluated in a receptor binding assay where a subset of compounds showed comparable potency to the agonists serotonin and 5- methoxytryptamine. Structure-activity analyses have highlighted promising avenues for further synthetic work and binding modes were proposed by docking these compounds into a homology model of the 5-HT4 receptor. Keywords: 5-HT4 ligands, serotonin, tryptamine, 5-HT4 receptor, medicinal chemistry
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