期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 16, 期 1, 页码 144-156出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2007.10.003
关键词
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A novel class of potent CCR3 receptor antagonists were designed and synthesized starting from N-1-[(6-fluoro-2-naphthyl)methyl]piperidin-4-yl}benzamide (1),which was found by subjecting our chemical library to high throughput screening (HTS). The CCR3 inhibitory activity of the synthesized compounds against eotaxin-induced Ca2+ influx was evaluated using CCR3-expressing preB cells. Systematic chemical modifications of I revealed that the 6-fluoro-2-naphthylmethyl moiety was essential for CCR3 inhibitory activity in this new series of CCR3 antagonists. Further structural modifications of the benzamide and piperidine moieties of 1 led to the identification of N-{8-[(6-fluoro-2-naphthyl)methyl]-8-azabicyclo[3.2.1]oct-3- yl} biphenyl-2-carboxamide (31) as a potent CCR3 antagonist with an IC50 value of 0.020 mu M. (C) 2007 Elsevier Ltd. All rights reserved.
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