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Substituted dipiperidine alcohols as potent CCR2 antagonists.
Xia, Mingde; Hou, Cuifen; Demong, Duane; Pollack, Scott; Pan, Meng; Brackley, James; Singer, Monica; Matheis, Michele; Cavender, Druie; Wachter, Michael.
Affiliation
  • Xia M; Drug Discovery, Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 8 Clarke Drive, Cranbury, NJ 08512, USA. mxia@prdus.jnj.com
Bioorg Med Chem Lett ; 18(12): 3562-4, 2008 Jun 15.
Article in En | MEDLINE | ID: mdl-18487045
ABSTRACT
The synthesis and biological evaluation of a series of substituted dipiperidine alcohols are described. Structure-activity relationship studies led to the discovery of potent CCR2 antagonists displaying IC(50) values in the nanomolar or subnanomolar range. The cinnamoyl compounds had higher binding affinities than the corresponding urea analogs.
Subject(s)

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Piperidines / Alcohols / Receptors, CCR2 Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2008 Document type: Article Affiliation country:

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Piperidines / Alcohols / Receptors, CCR2 Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2008 Document type: Article Affiliation country: