On November 26, 2012, Cavallaro, Cullen L.; Briceno, Stephanie; Chen, Jing; Cvijic, Mary Ellen; Davies, Paul; Hynes, John; Liu, Rui-Qin; Mandlekar, Sandhya; Rose, Anne V.; Tebben, Andrew J.; Van Kirk, Katy; Watson, Andrew; Wu, Hong; Yang, Guchen; Carter, Percy H. published an article.Computed Properties of 39512-49-7 The title of the article was Discovery and Lead Optimization of a Novel Series of CC Chemokine Receptor 1 (CCR1)-Selective Piperidine Antagonists via Parallel Synthesis. And the article contained the following:
A series of novel, potent CCR1 inhibitors was developed from a moderately active hit using an iterative parallel synthesis approach. The initial hit (composed of three subunits: an amine, a central amino acid, and an N-terminal cap) became the basis for a series of parallel chem. libraries designed to generate SAR data. Libraries were synthesized that explored each of the three subunits; the CCR1 binding data obtained revealed the following: changes to the amine are not well tolerated; small alkylamino acids are preferred in the center of the mol.; substitutions at the N-terminus are generally well tolerated. These data were used to drive the optimization of the series, ultimately providing a lead with a CCR1 binding IC50 of 28 nM (48). This lead demonstrates high selectivity for CCR1 over other CCR-family members, high microsomal stability, and good pharmacokinetics in mice. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Computed Properties of 39512-49-7
The Article related to structure activity preparation chemokine receptor ccr1 antagonist, Pharmacology: Structure-Activity and other aspects.Computed Properties of 39512-49-7
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem