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Gardner DS Santella JB Tebben AJ Batt DG Ko SS Traeger SC Welch PK Wadman EA Davies P Carter PH Duncia JV 《Bioorganic & medicinal chemistry letters》2008,18(2):586-595
Conformational analysis of the 3-benzylpiperidine in CCR3 antagonist clinical candidate 1 (BMS-639623) predicts that the benzylpiperidine may be replaced by acyclic, conformationally stabilized, anti-1,2-disubstituted phenethyl- and phenpropylamines. Ab initio calculations, enantioselective syntheses, and evaluation in CCR3 binding and chemotaxis assays of anti-1-methyl-2-hydroxyphenethyl- and phenpropylamine-containing CCR3 antagonists support this conformational correlation. 相似文献