127944-63-2Relevant articles and documents
Water-Soluble Renin Inhibitors: Design of a Subnanomolar Inhibitor with a Prolonged Duration of Action
Rosenberg, Saul H.,Woods, Keith W.,Sham, Hing L.,Kleinert, Hollis D.,Martin, Donald L.,et al.
, p. 1962 - 1969 (2007/10/02)
Incorporation of nonreactive polar functionalities at the C- and N-termini of renin inhibitors led to the development of a subnanomolar compound (21) with millimolar solubility.This inhibitor demonstrated excellent efficacy and a long duration of action upon intravenous administration to monkeys.While activity was also observed intraduodenally, a comparison of the blood pressure responses indicated low bioavailability.Subsequent experiments in rats showed that, although the compound was absorbed from the gastrointrestinal tract, extensive liver extraction severely limited bioavailability.
