II. SAR studies of pyridyl-piperazinyl-piperidine derivatives as CXCR3 chemokine antagonists.

Autor: Shao Y; Ligand Pharmaceuticals, Cranbury, NJ 08512, USA. joe.shao@primera-corp.com, Anilkumar GN, Carroll CD, Dong G, Hall JW 3rd, Hobbs DW, Jiang Y, Jenh CH, Kim SH, Kozlowski JA, McGuinness BF, Rosenblum SB, Schulman I, Shih NY, Shu Y, Wong MK, Yu W, Zawacki LG, Zeng Q
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Mar 01; Vol. 21 (5), pp. 1527-31. Date of Electronic Publication: 2010 Dec 28.
DOI: 10.1016/j.bmcl.2010.12.114
Abstrakt: The structure-human CXCR3 binding affinity relationship of a series of pyridyl-piperazinyl-piperidine derivatives was explored. The optimization campaign highlighted the pronounced effect of 2'-piperazine substitution on CXCR3 receptor affinity. Analog 18j, harboring a 2'(S)-ethylpiperazine moiety, exhibited a human CXCR3 IC(50) of 0.2 nM.
(Copyright © 2011 Elsevier Ltd. All rights reserved.)
Databáze: MEDLINE
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