328248-31-3Relevant academic research and scientific papers
New 1-aryl-3-substituted propanol derivatives as antimalarial agents
Perez-Silanes, Silvia,Berrade, Luis,Garcia-Sanchez, Rory N.,Mendoza, Adela,Galiano, Silvia,Perez-Solorzano, Berta Martin,Nogal-Ruiz, Juan J.,Martinez-Fernandez, Antonio R.,Aldana, Ignacio,Monge, Antonio
experimental part, p. 4120 - 4135 (2010/03/04)
This paper describes the synthesis and in vitro antimalarial activity against a P. falciparum 3D7 strain of some new 1-aryl-3-substituted propanol derivatives. Twelve of the tested compounds showed an IC50 lower than 1 μM. These compounds were
New 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives, with dual action at 5-HT1A serotonin receptors and serotonin transporter, as a new class of antidepressants
Martínez-Esparza,Oficialdegui,Pérez-Silanes,Heras,Orús,Palop,Lasheras,Roca,Mourelle,Bosch,Del Castillo,Tordera,Del Río,Monge
, p. 418 - 428 (2007/10/03)
In a search toward new and efficient antidepressants, 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives were designed, synthesized, and evaluated for 5-HT reuptake inhibition and 5-HT1A receptor antagonism. This dual pharmacological profile should lead, in principle, to a rapid and pronounced enhancement in serotoninergic neurotransmission and consequently to a more efficacious treatment of depression. The design was based on coupling structural moieties related to inhibition of serotonin reuptake, such as γ-phenoxypropylamines, to arylpiperazines, typical 5-HT1A ligands. In binding studies, several compounds showed affinity at the 5-HT transporter and 5-HT1A receptors. Antidepressant-like activity was initially assayed in the forced swimming test with those compounds with Ki 1A receptor. Furthermore, the antidepressant-like properties of 12f, 28a, and 28b, which exhibited 5-HT1A receptor antagonistic property in the latter study, were also evaluated in the learned helplessness test in rats. Among these three compounds, 28b (1-benzo[b]thiophene-3-yl)-3-[4-(2-methoxyphenyl)-1-ylpropan-1-ol) showed the higher affinity at both the 5-HT transporter and 5-HT1A receptors (Ki = 20 nM in both cases) and was also active in the other pharmacological tests. Such a pharmacological profile could lead to a new class of antidepressants with a dual mechanism of action and a faster onset of action.
