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Substituted dipiperidine alcohols as potent CCR2 antagonists |
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| Authors: | Xia Mingde Hou Cuifen Demong Duane Pollack Scott Pan Meng Brackley James Singer Monica Matheis Michele Cavender Druie Wachter Michael |
| Affiliation: | Drug Discovery, Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 8 Clarke Drive, Cranbury, NJ 08512, USA. mxia@prdus.jnj.com |
| 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. |
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