期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 6, 期 4, 页码 439-444出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml500505q
关键词
Chemokine; GPCR; dual antagonist; inflammation
资金
- Bristol-Myers Squibb Company
We describe the hybridization of our previously reported acyclic and cyclic CC chemokine receptor 2 (CCR2) antagonists to lead to a new series of dual antagonists of CCR2 and CCRS. Installation of a gamma-lactam as the spacer group and a quinazoline as a benzamide mimetic improved oral bioavailability markedly. These efforts led to the identification of 13d, a potent and orally bioavailable dual antagonist suitable for use in both murine and monkey models of inflammation.
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