Whitehead Brent R, Lo Michael M-C, Ali Amjad, Park Min K, Hoyt Scott B, Xiong Yusheng, Cai Jiaqiang, Carswell Emma, Cooke Andrew, MacLean John, Ratcliffe Paul, Robinson John, Bennett D Jonathan, Clemas Joseph A, Wisniewski Tom, Struthers Mary, Cully Doris, MacNeil Douglas J
MRL, Rahway, NJ 07065, USA.
MRL, Rahway, NJ 07065, USA.
Bioorg Med Chem Lett. 2017 Jan 15;27(2):143-146. doi: 10.1016/j.bmcl.2016.12.003. Epub 2016 Dec 2.
The inhibition of aldosterone synthase (CYP11B2) may be an effective treatment of hypertension and heart failure, among other ailments. Previously reported benzimidazole CYP11B2 inhibitors led the way for bioisosteric imidazopyridines that are both potent and selective over CYP11B1.
醛固酮合酶(CYP11B2)的抑制作用可能是治疗高血压、心力衰竭及其他疾病的有效方法。先前报道的苯并咪唑类CYP11B2抑制剂为具有生物电子等排性的咪唑并吡啶类化合物开辟了道路,这类化合物对CYP11B1具有强效且选择性的抑制作用。