N-(α-Hydroxyalkanoyl) Derivatives of Leu-Val-Phe-OCH3as Inhibitors of Renin

Rodney L. Johnson

Research output: Contribution to journalArticlepeer-review

11 Scopus citations

Abstract

The following N-(α-hydroxyalkanoyl) derivatives of Leu-Val-Phe-OCH3 were synthesized and tested for their ability to inhibit human amniotic renin: D- and L-α-hydroxyisocaproyl-Leu-Val-Phe-OCH3, D- and L-α-hydroxvisovaleryl-Leu-Val-Phe-OCH3, L-2-hydroxy-3-phenylpropanoyl-Leu-Val-Phe-OCH3, and D- and L-α-hydroxyphenylacetyl-Leu-Val-Phe-OCH3. Analysis of the compounds through the use of Dixon plots showed all of the compounds to be competitive inhibitors of renin. All but D-α-hydroxyisovaleryl-Leu-Val-Phe-OCH3were found to be more active than the known tetrapeptide inhibitor Leu-Leu-Val-Phe-OCH3(1). The two most active compounds of the series were L-α-hydroxyisocaproyl-Leu-Val-Phe-OCH3(Ki= 0.23 mM) and L-α-hydroxyisovaleryl-Leu-Val-Phe-OCH3(Ki= 0.3 mM).

Original languageEnglish (US)
Pages (from-to)666-669
Number of pages4
JournalJournal of medicinal chemistry
Volume23
Issue number6
DOIs
StatePublished - Jan 1 1980

Fingerprint Dive into the research topics of 'N-(α-Hydroxyalkanoyl) Derivatives of Leu-Val-Phe-OCH<sub>3</sub>as Inhibitors of Renin'. Together they form a unique fingerprint.

Cite this