Journal of Clinical & Experimental Pharmacology

Boron-containing compounds as ACE/AChE dual inhibitors against hypertension

17^th International Conference on PHARMACOLOGY AND DRUG DISCOVERY

June 15-16, 2023 | Rome, Italy

Alina Barquet Nieto

ESM - Higher School of Medicine �?? IPN, Mexico

Scientific Tracks Abstracts: J Clin Exp Pharmacol

Abstract:

Statement of the problem: Currently, antihypertensive treatment includes mono-target drugs, but considering this disease has a very diverse etiology these drugs are not satisfactory, since monotherapies often do not achieve the desired efficacy leading to increase doses or combine different drugs to improve the antihypertensive effect, which develop adverse effects. Multitarget treatment could reduce the appearance of adverse effects and in turn avoid drug interactions. Boroncontaining compounds have been known for more than a century, increasing interest in scientific research due to their possible use in treatments as antibiotics, antiseptics agents, antihypertensives. Methodology and Theoretical Orientation: Considering previous pharmacological activity of boroxazolidones, the aim of this investigation was to design and synthesize a series of boroxazolidones derived from α-amino acids, and evaluate their antihypertensive effect (in silico, in vitro and in vivo) as ACE/AChE inhibitors to determine the best compounds for this treatment. Findings: According to in silico studies, BXZ-His, BXZLys, BXZ Orn, BXZ-Phe and BXZ-Pro were selected as the most promising ACE and AChE inhibitors. After synthesis, these molecules were tested in vitro, to study the inhibitory activity on ACE and AChE. Finally, BXZ-Lys and BXZ-His were tested in vivo in spontaneously hypertensive rats. Conclusion & Significance: BXZ-LYS significantly decreased systolic, diastolic, and mean arterial pressure, being more potent than the ACE inhibitor drug, captopril.

Biography :

Alina Barquet Nieto is a PhD student in Medicine Research at the Higher School of Medicine of the National Polytechnic Institute. She is a Biologist Pharmaceutical Chemist by profession with a Master of Science in Pharmacology