Synthesis and Docking of Novel 3-Indolylpropyl Derivatives as New Polypharmacological Agents Displaying Affinity for 5-HTb>1A b>R/SERT
详细信息 查看全文
- 作者：Herná ; n Pessoa-Mahana ; Paul Silva-Matus ; C. David Pessoa-Mahana ; Hery Chung ; Patricio Iturriaga-Vá ; squez ; Gabriel Quiroz ; Patricia Mö ; ller-Acuñ ; a ; Gerald Zapata-Torres ; Claudio Saitz-Barrí ; a ; Ramiro Araya-Maturana and Miguel Reyes-Parada
- 刊名：Archiv der Pharmazie
- 出版年：2017
- 出版时间：January 2017
- 年：2017
- 卷：350
- 期：1
- 全文大小：1809K
- ISSN：1521-4184
文摘
A series of novel 3-indolylpropyl derivatives was synthesized and evaluated for their binding affinities at the serotonin-1A receptor subtype (5-HTb>1A b>R) and the 5-HT transporter (SERT). Compounds <b>11bb> and <b>14bb> exhibited the highest affinities at the 5-HTb>1A b>R (Kb>i b> = 43 and 56 nM), whereas compounds <b>11cb> and <b>14ab> were the most potent analogs at the SERT (Kb>i b> = 34 and 17 nM). On the other hand, compounds <b>14bb> and <b>11db> 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.