2015
DOI: 10.3109/14756366.2015.1054820
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Abstract: Carbonic anhydrases (CAs, EC 4.2.1.1), which are involved in a variety of physiological and pathological processes, are ubiquitous metalloenzymes mainly catalyzing the reversible hydration of carbon dioxide (CO 2 ) to bicarbonate (HCO À 3 ) and proton (H + ). In this study, a dozen of bromophenol derivatives (1-12) were evaluated as metalloenzyme CA (EC 4.2.1.1) inhibitors against the human carbonic anhydrase isoenzymes I and II (hCA I and II). Cytosolic hCA I and II isoenzymes were effectively inhibited by br… Show more

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Cited by 109 publications
(75 citation statements)
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“…1,2 The reversible hydration of carbon dioxide (CO 2 ) to form bicarbonate (HCO 3 À ) and protons (H + ) is a simple but very important chemical reaction that can be performed by various classes of carbonic anhydrases (CAs, EC 4.2.1.1). [3][4][5][6] The interconversion of CO 2 and HCO 3 À is spontaneously balanced to maintain the equilibrium between dissolved inorganic CO 2 , the highly unstable carbonic acid (H 2 CO 3 ) and carbonate (CO 3 2À ) of which HCO 3 À is physiologically the most important species (due to the physiological pH values). Indeed, bicarbonate is a substrate for several carboxylation enzymes involved in biosynthetic pathways such as biosynthesis of urea, glucose, fatty acids and possibly nucleotides [7][8][9][10] .…”
Section: Introductionmentioning
confidence: 99%
See 1 more Smart Citation
“…1,2 The reversible hydration of carbon dioxide (CO 2 ) to form bicarbonate (HCO 3 À ) and protons (H + ) is a simple but very important chemical reaction that can be performed by various classes of carbonic anhydrases (CAs, EC 4.2.1.1). [3][4][5][6] The interconversion of CO 2 and HCO 3 À is spontaneously balanced to maintain the equilibrium between dissolved inorganic CO 2 , the highly unstable carbonic acid (H 2 CO 3 ) and carbonate (CO 3 2À ) of which HCO 3 À is physiologically the most important species (due to the physiological pH values). Indeed, bicarbonate is a substrate for several carboxylation enzymes involved in biosynthetic pathways such as biosynthesis of urea, glucose, fatty acids and possibly nucleotides [7][8][9][10] .…”
Section: Introductionmentioning
confidence: 99%
“…Therefore, there is a growing interest in natural and safer antioxidants for food applications, and a growing trend in consumer preferences towards natural antioxidants, all of which have given impetus to the attempts to explore new and safer sources of antioxidants [65][66][67] . The interest on the synthesis of new such heterocyclic compounds, containing multifunctional nitrogen and sulfur atoms within the ring, and their application as antimicrobial and antioxidant agents 68 , prompted us to design the new cyclic thioureas (1)(2)(3)(4)(5)(6)(7)(8), which were obtained for the first time by us based on using trifluoroacetic acid (TFAA) as catalyst ( Figure 1).…”
Section: Introductionmentioning
confidence: 99%
“…In this method, changes in absorbance were recorded during 3 min at 25 C. P-nitrophenylacetate (NPA) was used as substrate and converted by both isoenzymes to p-nitrophenolate ion. These activity determinations are described in detail in our previous studies 77 . For determination of protein quantity, Bradford method was used during the purification steps 78 .…”
Section: Biochemical Studiesmentioning
confidence: 99%
“…In mammals, CA II, which generally exists in red blood cells in lower concentrations, has approximately 10 times higher activity compare with CA I [99][100][101][102] . Cytosolic hCA I isoenzyme is ubiquitously expressed in body, and available in high concentrations in blood and gastrointestinal tract.…”
Section: Biological Activitymentioning
confidence: 99%