Design and synthesis of novel small molecule CCR2 antagonists: Evaluation of 4-aminopiperidine derivatives |
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| Institution: | 1. Alexandru Ioan Cuza University of Iasi, Faculty of Physics, 11 Carol I Blvd, RO-700506 Iasi, Romania;2. Alexandru Ioan Cuza University, Faculty of Orthodox Theology, 42 Closca Street, RO-700087 Iasi, Romania |
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| Abstract: | A novel N-(2-oxo-2-(piperidin-4-ylamino)ethyl)-3-(trifluoromethyl)benzamide series of human CCR2 chemokine receptor antagonists was identified. With a pharmacophore model based on known CCR2 antagonists a new core scaffold was designed, analogues of it synthesized and structure–affinity relationship studies derived yielding a new high affinity CCR2 antagonist N-(2-((1-(4-(3-methoxyphenyl)cyclohexyl)piperidin-4-yl)amino)-2-oxoethyl)-3-(trifluoromethyl)benzamide. |
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| Keywords: | CCR2 Chemokine Antagonist 4-Aminopiperidine |
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