N-[2-(茚满-1-基)-3-巯基丙酰基]氨基酸作为三种血管肽酶（中性内肽酶、血管紧张素转换酶、内皮素转换酶）的高效抑制剂：体外和体内活性
N-[2-(Indan-1-yl)-3-mercapto-propionyl] amino acids as highly potent inhibitors of the three vasopeptidases (NEP, ACE, ECE): In vitro and In vivo activities.
作者信息
Inguimbert Nicolas, Poras Hervé, Teffo Franck, Beslot Françoise, Selkti Mohamed, Tomas Alain, Scalbert Elizabeth, Bennejean Caroline, Renard Pierre, Fournié-Zaluski Marie-Claude, Roques Bernard-Pierre
机构信息
Département de Pharmacochimie Moléculaire et Structurale, U266 INSERM, UMR 8600 CNRS, UFR des Sciences Pharmaceutiques et Biologiques, 4, avenue de l'observatoire, 75270 Cedex 06, Paris, France.
出版信息
Bioorg Med Chem Lett. 2002 Aug 5;12(15):2001-5. doi: 10.1016/s0960-894x(02)00248-2.
We have previously reported the design of a lead compound 1a for the joint inhibition of neprilysin (NEP, EC 3.4.24.11), angiotensin converting enzyme (ACE, EC 3.4.15.1) and endothelin converting enzyme (ECE-1, EC 3.4.24.71), three metallopeptidases which are implicated in the regulation of fluid homeostasis and vascular tone. We report here the synthesis and biological activities of analogues derived from this lead with inhibitory potencies in the nanomolar range for the three enzymes. Compounds 8b and 15c are the most potent triple inhibitors described to date.
我们之前报道过一种先导化合物1a的设计，该化合物可联合抑制中性肽链内切酶（NEP，EC 3.4.24.11）、血管紧张素转换酶（ACE，EC 3.4.15.1）和内皮素转换酶（ECE-1，EC 3.4.24.71），这三种金属肽酶参与了体液平衡和血管张力的调节。我们在此报告了源自该先导化合物的类似物的合成及生物活性，这些类似物对这三种酶的抑制效力在纳摩尔范围内。化合物8b和15c是迄今为止描述的最有效的三联抑制剂。
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