新型吲哚类磷酸二酯酶4（PDE4）抑制剂系列I的合成与生物学评价
The synthesis and biological evaluation of a novel series of indole PDE4 inhibitors I.
作者信息
Hulme C, Moriarty K, Miller B, Mathew R, Ramanjulu M, Cox P, Souness J, Page K M, Uhl J, Travis J, Huang F C, Labaudiniere R, Djuric S W
机构信息
Rhône-Poulenc Rorer Central Research, Collegeville, PA 19426, USA.
出版信息
Bioorg Med Chem Lett. 1998 Jul 21;8(14):1867-72. doi: 10.1016/s0960-894x(98)00324-2.
This communication describes the synthesis and in vitro evaluation of a novel potent series of phosphodiesterase type (IV) (PDE4) inhibitors. The compounds described contain an indole moiety which replaces the 'rolipram-like' 3-methoxy-4-cyclopentoxy motif. Several of the compounds presented possess low nanomolar IC50's for PDEIV inhibition. In vivo activities determined from measurement of serum TNF-alpha levels in LPS challenged mice (mouse endotoxemia model) are also reported.
本通讯描述了一系列新型强效磷酸二酯酶IV（PDE4）抑制剂的合成及体外评价。所描述的化合物含有一个吲哚部分，其取代了“咯利普兰样”的3-甲氧基-4-环戊氧基基序。所展示的几种化合物对PDEIV抑制的IC50值低至纳摩尔级别。还报告了通过测量脂多糖攻击小鼠（小鼠内毒素血症模型）血清中TNF-α水平所确定的体内活性。
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