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SCOZZAFAVA, ANDREA +2 more
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Novel Carbonic Anhydrase Inhibitors
Future Medicinal Chemistry, 2021Abstract
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Topical carbonic anhydrase inhibitors
Journal of Medicinal Chemistry, 1984Ethoxzolamide and several derivatives (1-6) were synthesized and evaluated for carbonic anhydrase inhibition (CAI), solubility, pKa, distribution, and corneal permeability. The 6-hydroxy (5) and, particularly, the 6-chloro (6) analogues have the best combination of properties for penetrating the site of action and reducing intraocular pressure.
R D, Schoenwald +3 more
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Hydroxyurea is a carbonic anhydrase inhibitor
Bioorganic & Medicinal Chemistry, 2003The interaction of hydroxyurea with the cytosolic isozymes of carbonic anhydrase (CA), hCA I and hCA II has been investigated by means of kinetic and spectroscopic techniques. Hydroxyurea acts as a weak, non-competitive inhibitor of both isozymes, for the 4-nitrophenyl acetate esterase activity, with inhibition constants around 0.1 mM for both isozymes.
SCOZZAFAVA, ANDREA +1 more
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Sulfonylmethanesulfonamide inhibitors of carbonic anhydrase
Journal of Medicinal Chemistry, 1993A series of sulfonylmethanesulfonamide derivatives is described, which are inhibitors of carbonic anhydrase (CA). The most potent of these is the racemic fluoro sulfone 9, which inhibits carbon dioxide hydration catalyzed by human CA II (CA-II) with an IC50 of 3 nM.
T H, Scholz +7 more
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Topical carbonic anhydrase inhibitors
Current Opinion in Ophthalmology, 1997Dorzolamide, a topically active carbonic anhydrase inhibitor, is an effective new glaucoma medication that creates a decrease in intraocular pressure similar to that produced by beta-blockers. When beta-blockers are contraindicated, dorzolamide may be used as a first-line therapy.
D M, Talluto, T B, Wyse, T, Krupin
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Bioorganic & Medicinal Chemistry Letters, 2010
Carbonic anhydrases (CAs, EC 4.2.1.1) are widespread enzymes in all organisms, catalyzing CO2 hydration to bicarbonate and protons. Their inhibition is exploited clinically for decades for various classes of diuretics and systemically acting antiglaucoma agents.
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Carbonic anhydrases (CAs, EC 4.2.1.1) are widespread enzymes in all organisms, catalyzing CO2 hydration to bicarbonate and protons. Their inhibition is exploited clinically for decades for various classes of diuretics and systemically acting antiglaucoma agents.
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Antiobesity Carbonic Anhydrase Inhibitors
Current Topics in Medicinal Chemistry, 2007Few pharmacological approaches for the treatment of obesity exist at this time, and most of them are unsatisfactory, whereas this disease is widespread both in the developed and developing world. Novel effective approaches are needed for the development of antiobesity agents possessing different mechanisms of action.
G. D. Simone, SUPURAN, CLAUDIU TRANDAFIR
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Carborane‐Based Carbonic Anhydrase Inhibitors
Angewandte Chemie International Edition, 2013CA inhibitors: Human carbonic anhydrases (CAs) are diagnostic and therapeutic targets. Various carborane cages are shown to act as active-site-directed inhibitors, and substitution with a sulfamide group and other substituents leads to compounds with high selectivity towards the cancer-specific isozyme IX.
Brynda, J. (Jiří) +8 more
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Safety of carbonic anhydrase inhibitors
Expert Opinion on Drug Safety, 2014Carbonic anhydrase (CA) inhibitors have an impressive safety record despite the multiple functions that CA isozymes serve because they are not fully inhibited with most dosing. While reducing the targeted CA-dependent process sufficiently for disease control, residual activity and uncatalyzed rates in combination with compensations are adequate to ...
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