季铵取代的磷酸二酯酶IV抑制剂II：新型γ-内酰胺系列的合成与体外评价
Quaternary substituted PDE IV inhibitors II: the synthesis and in vitro evaluation of a novel series of gamma-lactams.
作者信息
Hulme C, Moriarty K, Huang F C, Mason J, McGarry D, Labaudiniere R, Souness J, Djuric S
机构信息
Rhône-Poulenc Rorer Central Research, Collegeville, PA 19426, USA.
出版信息
Bioorg Med Chem Lett. 1998 Feb 17;8(4):399-404. doi: 10.1016/s0960-894x(98)00036-5.
PMID:9871693
Abstract
This communication describes the synthesis and in vitro evaluation of a novel potent series of phosphodiesterase type (IV) (PDE IV) inhibitors. Several of the quaternary substituted lactams presented possess low nanomolar IC50's for PDE IV inhibition.
摘要
本通讯描述了一系列新型强效磷酸二酯酶IV型（PDE IV）抑制剂的合成及体外评估。所呈现的几种季铵取代内酰胺对PDE IV抑制的半数抑制浓度（IC50）低至纳摩尔级别。
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