166809-58-1Relevant academic research and scientific papers
Identification of novel series of human CCR1 antagonists
Xie, Yun Feng,Sircar, Ila,Lake, Kirk,Komandla, Mallareddy,Ligsay, Kathleen,Li, Jian,Xu, Kui,Parise, Jason,Schneider, Lisa,Huang, Dingqiu,Liu, Juping,Sakurai, Naoki,Barbosa, Miguel,Jack, Rick
, p. 2215 - 2221 (2008/12/21)
A hit-to-lead optimization process was carried out on the high throughput screening hit compound 1 resulting in the identification of several potent and selective CCR1 receptor antagonists. Compound 37 shows the best overall profile with IC50 values of 100 nM in binding and functional assays.
CYCLIC AMIDE COMPOUNDS, PROCESS FOR THE PREPARATION OF THE SAME AND USES THEREOF
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, (2010/01/31)
A compound of the formula: wherein R1 is a hydrocarbon group, R2 is a hydrocarbon group having 2 or more carbon atoms, where R1 and R2 may in combination form, together with an adjacent nitrogen atom, a ring optionally having a substituent or substituents, R3 is a hydrocarbon group optionally having a substituent or substituents or a heterocyclic group optionally having a substituent or substituents, R4 is a hydrogen atom, a hydrocarbon group, a heterocyclic group and the like, E is a divalent chain hydrocarbon group and the like, G is CO or SO2, J is a nitrogen atom, a methine group and the like, and Q and R are each a divalent chain C1-3 hydrocarbon group and the like, and a salt thereof show a superior CCR5 antagonistic activity and are useful as agents for the prophylaxis or treatment of HIV infection of human peripheral blood mononuclear cells, particularly AIDS.
Synthesis and pharmacological activity of 2-(substituted phenyl)-3{2 or 3-[(4-substituted phenyl-4-hydroxy)piperidino]ethyl or propyl}-1,3- thiazolidin-4-ones
Diurno,Mazzoni,Capasso,Izzo,Bolognese
, p. 237 - 241 (2007/10/03)
A series of aryl-hydroxy-piperidinoalkyl-thiazolidinones was synthesized and evaluated to inhibit castor oil-induced diarrhea in mice. The dose dependent antidiarrheal activity of the most active compound 2-(p- nitrophenyl)-3-[2-[(4-(p-chlorophenyl)-4-hydroxy)piperidino]ethyl]-1,3- thiazolidin-4-one (6) was counteracted by naloxone, resulting comparable with that of loperamide, a μ opiate agonist.
