Iijima, Daisuke; Sugama, Hiroshi; Awai, Nobumasa; Takahashi, Yoichi; Togashi, Yuko; Takebe, Tohru; Xie, Jianshu; Shen, Jingkang; Ke, Ying; Akatsuka, Hidenori; Kawaguchi, Takayuki; Takedomi, Kei; Kashima, Akiko; Nishio, Masashi; Inui, Yosuke; Yoneda, Hikaru; Xia, Guangxin; Iijima, Toru published the artcile< Discovery of Novel 2-Carbamoyl Morpholine Derivatives as Highly Potent and Orally Active Direct Renin Inhibitors>, Electric Literature of 6482-24-2, the main research area is carbamoyl morpholine derivative preparation oral renin inhibitor hypertension.
The renin-angiotensin-aldosterone system (RAAS) plays a key role in the regulation of blood pressure. Renin, the first and rate-limiting enzyme of the RAAS, is an attractive target for the treatment of hypertension and cardiovascular/renal diseases. Therefore, various direct renin inhibitors (DRIs) have been researched over recent decades; however, most exhibited poor pharmacokinetics and oral bioavailability due to the peptidomimetic or nonpeptidomimetic structures with a mol. weight (MW) of >600, and only aliskiren is approved. This study introduces a novel class of DRIs comprised of a 2-carbamoyl morpholine scaffold. These compounds have a nonpeptidomimetic structure and a MW of <500. The representative compound 26 was highly potent despite not occupying S1′-S2′ sites or the opened flap region used by other DRIs and exerted a significant antihypertensive efficacy via oral administration on double transgenic mice carrying both the human angiotensinogen and the human renin genes. ACS Medicinal Chemistry Letters published new progress about Antihypertensives. 6482-24-2 belongs to class ethers-buliding-blocks, and the molecular formula is C3H7BrO, Electric Literature of 6482-24-2.
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem