Results 211 to 220 of about 42,053 (258)

Topical carbonic anhydrase inhibitors

Journal of Medicinal Chemistry, 1984
Ethoxzolamide 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, M G, Eller, J A, Dixson, C F, Barfknecht   +3 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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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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Dual Carbonic Anhydrase - Cyclooxygenase-2 Inhibitors

Current Topics in Medicinal Chemistry, 2007
Cyclooxygenase is a key enzyme responsible for metabolisation of arachidonic acid into prostaglandins and thromboxane. This enzyme is the target of non steroidal anti-inflammatory drugs (NSAIDs), used against inflammation and pain. The inducible COX-2 was associated with inflammatory conditions, whereas the constitutive form (COX-1) was responsible for
J. Dogné, A. Thiry, D. Pratico, B. Masereel, SUPURAN, CLAUDIU TRANDAFIR   +4 more
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Carbonic Anhydrase Inhibitors

1985
Inhibitors of carbonic anhydrase presently have a limited role in the treatment of epilepsy. Inorganic anions, such as I−, CN−, SH−, CNO−, SCN−, and Br−, and sulfonamides are inhibitors of the enzyme carbonic anhydrase (Maren 1967). Both bromides and sulfonamides have been used in the treatment of epilepsy in man.
J. E. Riggs, R. C. Griggs
openaire   +1 more source

Carbonic Anhydrase Inhibitors Drug Design

2013
Inhibition of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1) has pharmacologic applications in the field of antiglaucoma, anticonvulsant, antiobesity, and anticancer agents but is also emerging for designing anti-infectives (antifungal and antibacterial agents) with a novel mechanism of action. As a consequence, the drug design of CA inhibitors (
Robert, McKenna, Claudiu T, Supuran
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Patient Tolerance to Carbonic Anhydrase Inhibitors

American Journal of Ophthalmology, 1978
We evaluated carbonic anhydrase inhibitors in a crossover study with a placebo and random allocation of treatment administration. Drugs evaluated included acetazolamide tablets and Sequels, dichlorphenamide, ethoxzolamide, methazolamide, and an ascorbic acid placebo. The best tolerated drug was acetazolamide Sequels. Methazolamide was next.
P R, Lichter, L P, Newman, N C, Wheeler, O V, Beall   +3 more
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Boron-containing carbonic anhydrases inhibitors

Bioorganic Chemistry
Over the last decades, the medicinal chemistry of boron-based compounds has been extensively explored, designing valuable small molecule drugs to tackle diseases and conditions, such as cancer, infections, inflammatory and neurological disorders.
Giovannuzzi, Simone, Nikitjuka, Anna, Pereira Resende, Bruna Rafaela, Smietana, Michael, Nocentini, Alessio, Supuran, Claudiu T., Winum, Jean-Yves   +6 more
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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
openaire   +3 more sources