Discovery of TAK-272: A Novel, Potent, and Orally Active Renin Inhibitor

@inproceedings{Imaeda2016DiscoveryOT,
  title={Discovery of TAK-272: A Novel, Potent, and Orally
Active Renin Inhibitor},
  author={Yasuhiro Imaeda and Hidekazu Tokuhara and Yoshiyuki Fukase and Ray Kanagawa and Yumiko Kajimoto and Keiji Kusumoto and Mitsuyo Kondo and Gyorgy P Snell and Craig A. Behnke and Takanobu Kuroita},
  booktitle={ACS medicinal chemistry letters},
  year={2016}
}
The aspartic proteinase renin is an attractive target for the treatment of hypertension and cardiovascular/renal disease such as chronic kidney disease and heart failure. We introduced an S1' site binder into the lead compound 1 guided by structure-based drug design (SBDD), and further optimization of physicochemical properties led to the discovery of… CONTINUE READING