Key result
A series of 2-amino-4-thiazole-containing renin inhibitors, including PD 134672, demonstrated potent in vitro renin inhibition and oral blood pressure lowering activity in monkeys.
A novel series of 2-amino-4-thiazole-containing renin inhibitors demonstrated potent in vitro renin inhibition and oral blood pressure lowering efficacy in primate models.
Supports preclinical renin inhibitor development; leaves open translation to human hypertension trials.
A series of renin inhibitors was synthesized that contained a 2-amino-4-thiazolyl moiety at the P2 position. These derivatives are potent inhibitors of monkey renin in vitro and are selective in that they only weakly inhibit the closely related aspartic proteinase, bovine cathepsin D. Four compounds exhibited oral blood pressure lowering activity in high-renin normotensive monkeys. One of these compounds, 22 (PD 134672), was selected for further evaluation in renal hypertensive monkeys, on the basis of its superior efficacy and duration of action in the in vitro assays and the normotensive primate model.
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Patt et al. (1992) studied Hypertension (animal model). 2-amino-4-thiazole-containing renin inhibitors (e.g., PD 134672) was evaluated on In vitro renin inhibition and oral blood pressure lowering activity. A series of 2-amino-4-thiazole-containing renin inhibitors, including PD 134672, demonstrated potent in vitro renin inhibition and oral blood pressure lowering activity in monkeys.
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