Key result
Compound 1 matches captopril in reducing blood pressure via ACE inhibition, unlike compounds 2 and 3.
Compound 1 is a novel antihypertensive candidate that reduces blood pressure via ACE inhibition.
Compound 1 merits further preclinical study as an ACE inhibitor; leaves open translation to human hypertension.
Hypertension has been associated as a pathogenesis involved in the renin angiotensin system. The most commonly used drug to block the AT1R, is Losartan which has specific pharmacophore groups such as imidazole and biphenyl. However the development of new selective antagonists would be advantagous to improving the treatment of hypertension. We investigated innovative antihypertensive candidates1-3usingin vitroandin vivoassays. Although only Compound2showed low affinity to the AT1R, it had no effect on blood pressure. Compound1produced a reduction in blood pressure and this effect seems to be mediated through ACE inhibition and not the blockage of the AT1R. Compound1was able to inhibit the ACE activity in a similar way to captopril, while Compounds2and3showed no effect on the enzyme activity. Further studies need to be conducted to understand the mechanisms involved as well as signaling pathways.
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Ronchi et al. (2016) studied Hypertension. Compounds 1-3 vs. Captopril was evaluated on Blood pressure and ACE/AT1R activity. Compound 1 reduced blood pressure via ACE inhibition similar to captopril, whereas Compounds 2 and 3 had no effect on blood pressure or ACE activity.
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