Synthesis of N-(phosphonoacetyl)-dipeptide derivatives and evaluation of their antihypertensive activity |
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Authors: | G Osapay P K?rm?czy I Szilágyi J Kajtár B Kiss |
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Affiliation: | Research Institute of Chinoin Pharmaceutical and Chemical Works, L E?tv?s University, Budapest, Hungary. |
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Abstract: | A series of N-(phosphonoacetyl)-dipeptide derivatives was synthesized for pharmacological testing as antihypertensive compounds. Several of these compounds demonstrated a moderate antihypertensive effect in Wistar spontaneous hypertensive rats (SHR) with p.o. dosing. ACE inhibition by the compounds was studied using ACE from rat plasma and lung. Inhibitors containing esterified C-termini are pro-drugs and showed activity only for plasma ACE. |
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