QSARs on human carbonic anhydrase VA and VB inhibitors of some new not yet synthesized, substituted aromatic/heterocyclic sulphonamides as anti-obesity agent

Carbonic anhydrase inhibitors. Phenols incorporating 2- or 3-pyridyl-ethenylcarbonyl and tertiary amine moieties strongly inhibitSaccharomyces cerevisiaeβ-carbonic anhydrase

“…Five distinct genetic families (a-, b-, g-, -and z-CAs) encode such enzymes in organisms all over the phylogenetic tree [6][7][8][9][10][11][12][13][14][15] . CAs efficiently catalyze the simple but essential reaction between carbon dioxide and water, with generation of bicarbonate and protons, which is too slow without a catalyst at neutral pH values, by using a metal hydroxide as nucleophile, at nearly neutral pH values [10][11][12][13][14][15][16][17][18][19][20] . All chemical species involved in the CA-catalyzed reaction, carbon dioxide, bicarbonate and protons, are involved in many crucial physiologic processes and their perturbation may lead to dysfunctions [10][11][12][13][14][15][16][17][18][19][20] .…”

“…CAs efficiently catalyze the simple but essential reaction between carbon dioxide and water, with generation of bicarbonate and protons, which is too slow without a catalyst at neutral pH values, by using a metal hydroxide as nucleophile, at nearly neutral pH values [10][11][12][13][14][15][16][17][18][19][20] . All chemical species involved in the CA-catalyzed reaction, carbon dioxide, bicarbonate and protons, are involved in many crucial physiologic processes and their perturbation may lead to dysfunctions [10][11][12][13][14][15][16][17][18][19][20] . CAs also play important roles in fungi/yeasts, being involved in the CO 2 -sensing mechanism of these organisms and in their regulation of sexual development [1][2][3][4][5] .…”

Novel coumarins and benzocoumarins acting as isoform-selective inhibitors against the tumor-associated carbonic anhydrase IX

“…For this reason, exploring novel coumarin derivatives as CAIs, or compounds known in the literature but not yet investigated for this activity, is of interest in the design of isoform-selective pharmacological agents of this type. Indeed, CAIs have a range of applications as antiglaucoma, antiobesity, antiepileptic or diuretic agents [12][13][14][15][16][17][18][19][20][21][22][23][24][25][26] . Furthermore, inhibition of CAs from various bacteria or fungi may also lead to the development of antiinfectives based on CAIs 27,28 .…”

Carbonic anhydrases: from biomedical applications of the inhibitors and activators to biotechnological use for CO2 capture

“…All of them are essential molecules/ions in many important physiologic processes in all life kingdoms (Bacteria, Archaea and Eukarya), throughout the tree of life, and for this reason, relatively high amounts of these enzymes are present in different tissues/cell compartments of most investigated organisms [1][2][3][4][5][6][7][8][9][10] . Drugs interfering with the activity of the CAs have been clinically used for almost 60 years, most of them belonging to the sulfonamide class 1,3,9,10 . Inhibition of the CAs has pharmacologic applications in many fields, such as antiglaucoma, anticonvulsant, antiobesity, and anticancer agents/diagnostic tools, but their use is also emerging for designing anti-infectives, i.e., antifungal and antibacterial agents with a novel mechanism of action 1,3,[11][12][13] .…”

“…CAs are metalloenzymes, and they equilibrate the reaction between three simple but essential chemical species: CO 2 , bicarbonate and protons [1][2][3][4][5][6][7][8][9] . All of them are essential molecules/ions in many important physiologic processes in all life kingdoms (Bacteria, Archaea and Eukarya), throughout the tree of life, and for this reason, relatively high amounts of these enzymes are present in different tissues/cell compartments of most investigated organisms [1][2][3][4][5][6][7][8][9][10] .…”