193882-56-3Relevant articles and documents
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.
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.