5586-90-3Relevant academic research and scientific papers
Synergetic Effect of Monomer Functional Group Coordination in Catalytic Insertion Polymerization
Leicht, Hannes,G?ttker-Schnetmann, Inigo,Mecking, Stefan
, p. 6823 - 6826 (2017)
PhS- and PhNH-functionalized dienes are copolymerized efficiently with butadiene to stereoregular copolymers by [(mesitylene)Ni(allyl)][BArF4] (Ni-1). Overall polymerization rates and comonomer incorporations depend strongly on the l
Synthesis and pharmacological characterization of novel inverse agonists acting on the viral-encoded chemokine receptor US28
Hulshof, Janneke W.,Vischer, Henry F.,Verheij, Mark H.P.,Fratantoni, Silvina A.,Smit, Martine J.,de Esch, Iwan J.P.,Leurs, Rob
, p. 7213 - 7230 (2007/10/03)
G-protein coupled receptors encoded by viruses represent an unexplored class of potential drug targets. In this study, we describe the synthesis and pharmacological characterization of the first class of inverse agonists acting on the HCMV-encoded receptor US28. It is shown that replacement of the 4-hydroxy group of lead compound 1 with a methylamine group results in a significant 6-fold increase in affinity. Interestingly, increasing the rigidity of the spacer by the introduction of a double bond also leads to a significant increase in binding affinity compared to 1. These novel inverse agonists serve as valuable tools to elucidate the role of constitutive signaling in the pathogenesis of viral infection and may have therapeutic potential as leads for new antiviral drugs.
1-piperidines and Related Compounds, Potential Antipsychotic Agents with Low Cataleptogenic Profiles
Wise, Lawrence D.,Pattison, Ian C.,Butler, Donald E.,DeWald, Horace A.,Lewis, Edward P.,et al.
, p. 606 - 612 (2007/10/02)
On the basis of a structural model of the postsynaptic dopaminergic antagonist pharmacophore, a series of 1-piperidines and related compounds was synthesized and evaluated for potential antipsychotic activity.For a rapid measure of activity, the target compounds were initially screened in vitro for inhibition of haloperidol binding and in vivo in a test of locomotor activity.Behavioral efficacy of compounds identified from the initial screens was more accurately measured in rats by using a suppression of high base-line medial forebrain bundle self-stimulation test model.The propensity of these compounds for causing extrapyramidal side effects was evaluated by using a rat catalepsy method.On the basis of these test models, we have shown that the methine carbon of the 1-(4,4-diarylbutyl)piperidines can be advantageously replaced with a nitrogen atom.The 1-piperidines were less cataleptic than the corresponding 1-(4,4-diarylbutyl)piperidines.The compounds with the widest separation between efficacious dose and cataleptic dose are 8-propyl>-1-phenyl-1,3,8-triazaspirodecan-4-one (6), 1-propyl>-4-piperidinyl>-1,3-dihydro-2H-benzimidazol-2-one (11), 1-propyl>-1,2,3,6-tetrahydro-4-pyridinyl>-1,3-dihydro-2H-benzimidazol-2-one (22), and 1-propyl>-4-(2-methoxyphenyl)piperazine (26).
