728024-41-7Relevant academic research and scientific papers
Synthesis and Docking of Novel 3-Indolylpropyl Derivatives as New Polypharmacological Agents Displaying Affinity for 5-HT1AR/SERT
Pessoa-Mahana, Hernán,Silva-Matus, Paul,Pessoa-Mahana, C. David,Chung, Hery,Iturriaga-Vásquez, Patricio,Quiroz, Gabriel,M?ller-Acu?a, Patricia,Zapata-Torres, Gerald,Saitz-Barría, Claudio,Araya-Maturana, Ramiro,Reyes-Parada, Miguel
, (2017/01/10)
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 (Ki = 43 and 56 nM), whereas compounds 11c and 14a were the most potent analogs at the SERT (Ki = 34 and 17 nM). 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.
Domino cyclodimerization of indole-derived donor-acceptor cyclopropanes: One-step construction of the pentaleno[1,6-a,b]indole skeleton
Ivanova, Olga A.,Budynina, Ekaterina M.,Chagarovskiy, Alexey O.,Rakhmankulov, Eduard R.,Trushkov, Igor V.,Semeykin, Alexander V.,Shimanovskii, Nikolay L.,Melnikov, Mikhail Ya.
supporting information; experimental part, p. 11738 - 11742 (2011/11/29)
The fellowship of the rings: The previously undiscovered ability of indole-derived donor-acceptor cyclopropanes to involve four reaction centers simultaneously was revealed by their domino cyclodimerization (see scheme). This SnCl4-induced reac
