Alkylsulfone-containing trisubstituted cyclohexanes as potent and bioavailable chemokine receptor 2 (CCR2) antagonists |
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| Affiliation: | 1. Key Laboratory of Pathogenic Microbiology and Immunology, Institute of Microbiology, Chinese Academy of Sciences, Beijing 100101, China;2. College of Animal Science, Fujian Agriculture and Forestry University, Fuzhou 350002, China;3. School of Life Sciences, Anhui University, Hefei 230601, China |
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| Abstract: | We describe novel alkylsulfones as potent CCR2 antagonists with reduced hERG channel activity and improved pharmacokinetics over our previously described antagonists. Several of these new alkylsulfones have a profile that includes functional antagonism of CCR2, in vitro microsomal stability, and oral bioavailability. With this improved profile, we demonstrate that two of these antagonists, 2 and 12, are orally efficacious in an animal model of inflammatory recruitment. |
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| Keywords: | CCR2 CCR2 antagonist Chemokine antagonist GPCR |
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