Pettersen Daniel, Davidsson Öjvind, Whatling Carl
CVMD iMed, AstraZeneca R&D Mölndal, S-413 83 Mölndal, Sweden.
CVMD iMed, AstraZeneca R&D Mölndal, S-413 83 Mölndal, Sweden.
Bioorg Med Chem Lett. 2015 Jul 1;25(13):2607-12. doi: 10.1016/j.bmcl.2015.04.090. Epub 2015 May 6.
A number of FLAP inhibitors have been progressed to clinical trials for respiratory and other inflammatory indications but so far no drug has reached the market. With this Digest we assess the opportunity to develop FLAP inhibitors for indications beyond respiratory disease, and in particular for atherosclerotic cardiovascular disease. We also show how recently disclosed FLAP inhibitors have structurally evolved from the first generation FLAP inhibitors paving the way for new compound classes.
许多5-脂氧合酶激活蛋白(FLAP)抑制剂已进入针对呼吸系统和其他炎症适应症的临床试验,但到目前为止,尚无药物上市。在本综述中,我们评估了开发用于呼吸系统疾病以外适应症,特别是动脉粥样硬化性心血管疾病的FLAP抑制剂的机会。我们还展示了最近披露的FLAP抑制剂在结构上是如何从第一代FLAP抑制剂演变而来的,为新的化合物类别铺平了道路。