Results 201 to 210 of about 695,880 (253)

Hydroxyurea is a carbonic anhydrase inhibitor

Bioorganic & Medicinal Chemistry, 2003
The 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, SUPURAN, CLAUDIU TRANDAFIR   +1 more
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Carbonic anhydrase inhibitors

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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Sulfonylmethanesulfonamide inhibitors of carbonic anhydrase

Journal of Medicinal Chemistry, 1993
A 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, J M, Sondey, W C, Randall, H, Schwam, W J, Thompson, P J, Mallorga, M F, Sugrue, S L, Graham   +7 more
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Topical carbonic anhydrase inhibitors

Current Opinion in Ophthalmology, 1997
Dorzolamide, 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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Antiobesity Carbonic Anhydrase Inhibitors

Current Topics in Medicinal Chemistry, 2007
Few 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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Safety of carbonic anhydrase inhibitors

Expert Opinion on Drug Safety, 2014
Carbonic 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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Carborane‐Based Carbonic Anhydrase Inhibitors

Angewandte Chemie International Edition, 2013
CA 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), Mader, P. (Pavel), Šícha, V. (Václav), Fábry, M. (Milan), Poncová, K. (Kristýna), Bakardjiev, M. (Mario), Grüner, B. (Bohumír), Cígler, P. (Petr), Řezáčová, P. (Pavlína)   +8 more
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Carbonic Anhydrase Inhibitors as Anticonvulsant Agents

Current Topics in Medicinal Chemistry, 2007
Seizures are one of the most common neurological disorders in clinical medicine. Triggering mechanisms by which seizures form remain unclear, but are related to a rapid change in ionic composition, including an increase of intracellular potassium concentration and pH shifts within the brain.
A. Thiry, J. Dogné, SUPURAN, CLAUDIU TRANDAFIR, B. Masereel   +3 more
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Carbonic Anhydrase Inhibitors in Oncology

Tumor hypoxia and extracellular acidosis are hallmarks of the tumor microenvironment that promote cancer progression, metabolic adaptation, and resistance to therapy. Among the molecular mediators of these processes, carbonic anhydrase IX (CA IX) and carbonic anhydrase XII (CA XII) play central roles in maintaining intracellular pH homeostasis and ...
Claudiu T, Supuran, Andrea, Angeli
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Depression of Chloride Transport by Carbonic Anhydrase Inhibitors in the Absence of Carbonic Anhydrase

Nature, 1967
CARBONIC anhydrase is present in the frog gastric mucosa and fish gill which actively transport chloride, and it has been observed that carbonic anhydrase inhibitors of the sulphonamide type decrease net chloride active transport in these tissues1,2. Zadunaisky3 has reported that chloride is actively transported by the frog cornea, and 95–100 per cent ...
S, Kitahara, K R, Fox, C A, Hogben
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