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Phthalamide derivatives as ACE/AChE/BuChE inhibitors against cardiac hypertrophy: an in silico, in vitro, and in vivo modeling approach
This study aimed to synthesize three phthalamide derivatives (M-01, M-02, and M-03) and evaluate them as three-target (ACE/AChE/BuChE) inhibitors with the possible dual effect of reducing hypertension and r everting cardiac hypertrophy. After in silico and in vitro experiments, one compound was tested in vivo on rats. All three phthalamides were synthesized in good yields, showing good competitive inhibition of the three-target enzymes in silico and in vitro. M-01 (10 mg/kg) significantly reversed ca rdiomyocite hypertrophy (by 87.3%;p <  0.001) in the heart of spontaneous hypertensive rat (SHR) model. It was at l...
Source: Medicinal Chemistry Research - February 3, 2021 Category: Chemistry Source Type: research

Novel phthalamide derivatives as antihypertensive agents: rapid and clean synthesis, in silico and in vivo evaluation
AbstractHypertension is a prevalent progressive disorder and a key risk factor for cardiovascular disease, stroke, and kidney disease. Angiotensin-I-converting enzyme (ACE) inhibitors are the first-line drugs for treating hypertension, but they have many side effects. ACE is a zinc dipeptidyl carboxypeptidase that cleaves the decapeptide angiotensin-I to form the vasopressor angiotensin-II. Since the latter molecule is the main bioactive product of the renin –angiotensin system, its inhibition is a key strategy for hypertension therapy. The aim of this study was to conduct an in silico evaluation of a series of new phtha...
Source: Medicinal Chemistry Research - March 17, 2019 Category: Chemistry Source Type: research