Synthesis and Docking of Novel 3-Indolylpropyl Derivatives as New Polypharmacological Agents Displaying Affinity for 5-HT1AR/SERT

Pessoa-Mahana Hernan; Silva-Matus Paul; David Pessoa-Mahana C.; Chung Hery; Iturriaga-Vasquez Patricio; Quiroz Gabriel; Moller-Acuna Patricia; Zapata-Torres Gerald; Saitz-Barria Claudio; Araya-Maturana Ramiro; Reyes-Parada Miguel

首页> 外文期刊>Archiv der Pharmazie >Synthesis and Docking of Novel 3-Indolylpropyl Derivatives as New Polypharmacological Agents Displaying Affinity for 5-HT1AR/SERT

【24h】

Synthesis and Docking of Novel 3-Indolylpropyl Derivatives as New Polypharmacological Agents Displaying Affinity for 5-HT1AR/SERT

机译：新型3-吲哚基丙基衍生物的合成与对接为新的多酚肌动态剂，为5-HT1AR / SERT显示亲和力

获取原文

获取原文并翻译 | 示例

掌桥外文数据库（机构版） >>

开具论文收录证明 >>

文献代查 >>

页面导航

摘要
著录项
相似文献
相关主题

摘要

A series of novel 3-indolylpropyl derivatives was synthesized and evaluated for their binding affinities at the serotonin-1A receptor subtype (5-HT1AR) and the 5-HT transporter (SERT). Compounds 11b and 14b exhibited the highest affinities at the 5-HT1AR (K-i = 43 and 56nM), whereas compounds 11c and 14a were the most potent analogs at the SERT (K-i = 34 and 17nM). On the other hand, compounds 14b and 11d showed potent activity at both targets, displaying a profile that makes them promising leads for the search for novel potent ligands with a dual mechanism of action. Molecular docking studies in all the compounds unveiled relevant drug-target interactions, which allowed rationalizing the observed affinities.

机译：None

著录项

来源
《Archiv der Pharmazie》 |2017年第1期|共6页
作者
Pessoa-Mahana Hernan; Silva-Matus Paul; David Pessoa-Mahana C.; Chung Hery; Iturriaga-Vasquez Patricio; Quiroz Gabriel; Moller-Acuna Patricia; Zapata-Torres Gerald; Saitz-Barria Claudio; Araya-Maturana Ramiro; Reyes-Parada Miguel;
展开▼
作者单位

Univ Chile Dept Quim Org &

Fisicoquim Fac Ciencias Quim &

Farmaceut Casilla 233 Santiago 1;

Univ Chile Dept Quim Org &

Fisicoquim Fac Ciencias Quim &

Farmaceut Casilla 233 Santiago 1;

Pontificia Univ Catolica Chile Fac Quim Dept Farm Santiago Chile;

Pontificia Univ Catolica Chile Fac Quim Dept Farm Santiago Chile;

Univ La Frontera Fac Ingn &

Ciencias Dept Ciencias Quim &

Recursos Nat Temuco Chile;

Univ Chile Programa Doctorado Farmacol Santiago Chile;

Univ Talca Fac Ingn Ctr Bioinformat &

Simulac Mol Talca Chile;

Univ Chile Fac Ciencias Quim &

Farmaceut Dept Quim Inorgan &

Analit Santiago Chile;

Univ Chile Dept Quim Org &

Fisicoquim Fac Ciencias Quim &

Farmaceut Casilla 233 Santiago 1;

Univ Talca Inst Quim Recursos Nat Talca Chile;

Univ Santiago Chile Fac Ciencias Med Escuela Med Santiago Chile;

展开▼
收录信息
原文格式 PDF
正文语种 ger
中图分类药学;
关键词
Docking; 5-Hydroxytryptamine 1A receptor; Indole; Piperazinylpropylindole derivatives; Serotonin transporter;

机译：对接;5-羟基羟基胺1A受体;吲哚;哌嗪基丙基吲哚衍生物;血清素转运蛋白;

相似文献

外文文献
中文文献
专利

1. Synthesis,Biological Evaluation and Molecular Docking of Novel Phenylpyrimidine Derivatives as Potential Anticancer Agents [J] . JIN Bo, TAO Ye, YANG Hongliang 高等学校化学研究（英文版） . 2018,第006期
2. p-TSA-catalyzed one-pot synthesis and docking studies of some 5H-indeno1,2-bquinoline-9,11 (6H,10H)-dione derivatives as anticonvulsant agents [J] . Kamaal Ahmed, Balkrishna Dubey, Sayyed Nadeem, 中国化学快报（英文版） . 2016,第005期
3. Synthesis,Antimicrobial Activity,and Molecular Docking of Benzoic Hydrazide or Amide Derivatives Containing a 1,2,3-Triazole Group as Potential SDH Inhibitors [J] . Yue Ding, Ling Zhang, Song Yang, 中国化学（英文版） . 2021,第005期
4. Design, Synthesis, in VitroAntibacterial Activity, and Docking Studies of New Rhodanine Derivatives [J] . Aisha Abusetta, Jowhara Alumairi, Mariam Y. Alkaabi, 药物化学期刊（英文） . 2020,第001期
5. Synthesis and Docking of Novel 3-Indolylpropyl Derivatives as New Polypharmacological Agents Displaying Affinity for 5-HT1AR/SERT [J] . Pessoa-Mahana Hernan, Silva-Matus Paul, David Pessoa-Mahana C., Archiv der Pharmazie . 2017,第1期

机译：新型3-吲哚基丙基衍生物的合成与对接为新的多酚肌动态剂，为5-HT1AR / SERT显示亲和力
6. Synthesis, docking and pharmacological evaluation of novel homo- and hetero-bis 3-piperazinylpropylindole derivatives at SERT and 5-HT1A receptor [J] . Pessoa-MahanaH., González-LiraC., FierroA., Bioorganic and medicinal chemistry . 2013,第24期

机译：新型均一和杂双3-哌嗪基丙基吲哚衍生物在SERT和5-HT1A受体的合成，对接和药理学评估
7. Docking study, synthesis, and in vitro evaluation of fluoro-MADAM derivatives as SERT ligands for PET imaging. [J] . Mavel S, Vercouillie J, Garreau L, Bioorganic and medicinal chemistry . 2008,第19期

机译：氟-MADAM衍生物作为PET成像的SERT配体的对接研究，合成和体外评估。
8. Synthesis and Vitamin D Receptor Affinity of 16-Oxa Vitamin D3Derivatives-2 [C] . Ibe Kouta, Ogami Mayu, Yamada Takeshi 日本化学会春季年会 . 2020

机译：16-OXA维生素D3远序列-2的合成和维生素D受体亲和力-2
9. AFFINITY LABELING: I. SYNTHESIS, CHARACTERIZATION AND REACTIONS OF BROMOETHYL AMP DERIVATIVES. II. MODIFICATION OF DPN-ISOCITRATE DEHYDROGENASE BY KETOGLUTARATE DERIVATIVES [D] . BEDNAR, RODNEY ALLAN. 1982

机译：亲和力标签：I.溴乙基安培衍生物的合成，表征和反应。二。酮戊二酸衍生物对DPN-异柠檬酸脱氢酶的修饰
10. Synthesis and evaluation of arylpiperazines derivatives of 35-dioxo-(2H4H)-124-triazine as 5-HT1AR ligands [O] . J. S. Dileep Kumar, Vattoly J. Majo, Jaya Prabhakaran, -1

机译：35-二氧-（2H4H）-124-三嗪作为5-HT1AR配体的芳基哌嗪衍生物的合成和评价
11. Synthesis, Biological Properties and Comparative Molecular Docking Evaluation Studies of 1,3 and 1,4 Bis-Thiourea Derivatives as Potential Antimicrobial Resistant Agents [O] . Wan Sharifatun Handayani Wan Zullkiplee, Ferlicia Rasin, Ainaa Nadiah Abd Halim, 2021

机译：1,3和1,4双硫脲衍生物作为潜在抗微生物抗性剂的合成，生物学性能和对比分子对比评价研究
12. Synthesis of Amino Derivatives of Dithio Acids as Potential Radiation Protective Agents [R] . Foye, W. O. 1985

机译：二硫代氨基衍生物作为潜在辐射防护剂的合成

Synthesis and Docking of Novel 3-Indolylpropyl Derivatives as New Polypharmacological Agents Displaying Affinity for 5-HT1AR/SERT

摘要

著录项

相似文献

相关主题

期刊订阅