Lacombe Patrick, Deschênes Denis, Dubé Daniel, Dubé Laurence, Gallant Michel, Macdonald Dwight, Mastracchio Antony, Perrier Hélène, Charleson Stella, Huang Zheng, Laliberté France, Liu Susana, Mancini Joseph A, Masson Paul, Salem Myriam, Styhler Angela, Girard Yves
Merck Frosst Center for Therapeutic Research, PO Box 1005, Pointe Claire-Dorval, Que., Canada H9R 4P8.
Bioorg Med Chem Lett. 2006 May 15;16(10):2608-12. doi: 10.1016/j.bmcl.2006.02.043. Epub 2006 Mar 3.
Potent inhibitors of the human PDE IV enzyme are described. Substituted 8-arylquinoline analogs bearing nitrogen-linked side chain were identified as potent inhibitors based on the SAR described herein. The pharmacokinetic profile of the best analog and the in vivo efficacy in an ovalbumin-induced bronchoconstriction assay in conscious guinea pigs are reported.
本文描述了人磷酸二酯酶IV（PDE IV）的强效抑制剂。基于本文所述的构效关系（SAR），带有氮连接侧链的取代8-芳基喹啉类似物被鉴定为强效抑制剂。报道了最佳类似物的药代动力学特征以及在清醒豚鼠卵清蛋白诱导的支气管收缩试验中的体内疗效。
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