Abstract
In an effort to comprehensively characterize an antioxidant profile of 2-alkoxyphenylcarbamic acid-based compounds containing a 4´-(substituted phenyl)piperazin-1´-yl fragment, they were in vitro screened in the 2,2´-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) derived radical cation (ABTS•+) and ferric reducing antioxidant power (FRAP) assay using the UV/VIS spectrophotometry. The ABTS•+ scavenging (reducing) potential of 1-[3-(2-methoxyphenylcarbamoyl)oxy-2-hydroxypropyl]-4-(4-fluorophenyl)piperazin-1-ium chloride was found to be the most promising and it was comparable to the efficiency of the carvedilol reference drug. Moreover, that 4´-fluoro group-containing compound was regarded as more active than the atenolol standard. When testing the molecules´ power to reduce the ferric 2,4,6-tris (2-pyridyl)-s-triazine complex [Fe(III)(TPTZ)2]3+, the most prospective was 1-[3-(2-ethoxyphenylcarbamoyl)oxy-2-hydroxypropyl]-4-(4-fluorophenyl)piperazin-1-ium chloride. On the other hand, its Fe3+ reducing power was lower compared to both standards carvedilol and atenolol. The study discussed structure–antioxidant properties relationships considering electronic, steric and lipophilic features.
Highlights
Cardiovascular disease (CVD) is still the most common cause of death in Europe, causing almost twice as many deaths as cancer across the continent and places a substantial burden on the health care systems and economies of Europe
Following the chemical structure of currently in vitro screened compounds 1–4, their capability to scavenge a large nitrogen-centered and sterically-hindered blue-green radical cation ABTS+ and a colourless [Fe(III)(TPTZ)2]3+ complex could be dependent on: (i) electronic, steric and lipohydrophilic properties of the R2 substituent attached to the salt-forming moiety and (ii) a length of the R1 group of a lipophilic part (Table I)
The σ output for the 4 ́-F substituent (σ4 ́-F) was 0.06, the σ value related to the 3 ́-CF3 moiety (σ3 ́-CF3) was set to
Summary
Cardiovascular disease (CVD) is still the most common cause of death in Europe, causing almost twice as many deaths as cancer across the continent and places a substantial burden on the health care systems and economies of Europe. Mortality and morbidity from the CVD continue to have a major social and economic impact in Europe and significant inequalities are evident between countries. There have been major improvements in recent years on many measures of the CVD, these improvements have not been universal and substantial inequalities persist (Nichols et al, 2013; Townsend et al, 2015; Townsend et al, 2016). Notable evidence-based lifestyle interventions, as non-pharmacological approaches, leading to the changes in a diet, physical activity, and functional parameters can produce modest but clinically significant weight loss, reduce the prevalence of a type 2 diabetes mellitus and improve cardiovascular risk factors and mortality for the people, who are not overweight (Antala et al, 2008; Eguchi et al, 2014; Gillet et al, 2012; Kyselovičová et al, 2014; Loveman et al, 2011; Tibenská and Medeková, 2014). Several metabolites of carvedilol have been considered extremely strong anti-
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