Potent renin inhibitory peptides containing hydrophilic end groups.

We have synthesized a series of hydrophilic derivatives of the renin inhibitor U-71038, some of which improved the water solubility of the parent by a factor of >100. Within a factor of 10, all of these derivatives retained the potent in vitro human renin inhibitory activity of U-71038. Several at doses equimolar to U-71038, produced hypotensive responses in the rat of greater magnitude and longer duration than U-71038