Abstract
Oral bioavailability has been a formidable barrier to the development of drugs which mimic the structures of biologically active peptides. This report describes the discovery of potent renin inhibitors having high oral bioavailability and good plasma pharmacokinetics. These are substances derived by modification of the P4–P1’ sequence of angiotensinogen, the renin substrate. These results demonstrate a successful peptide mimetic approach to the design of orally bioavailable pharmacologically active agents.
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Hoover, D.J. et al. (1995). Discovery of Inhibitors of Human Renin with High Oral Bioavailability. In: Takahashi, K. (eds) Aspartic Proteinases. Advances in Experimental Medicine and Biology, vol 362. Springer, Boston, MA. https://doi.org/10.1007/978-1-4615-1871-6_21
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DOI: https://doi.org/10.1007/978-1-4615-1871-6_21
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