Carbonic Anhydrase Inhibitor

4-Acetylphenylboronic acid is a potent inhibitor of carbonic anhydrases II(CA II), with IC₅₀s of 246 μM and 281.40 μM for bovine CA II (bCA II) and human CA II (hCA II). 4-Acetylphenylboronic acid can be obtained via mechanochemistry and solvent evaporation. 4-Acetylphenylboronic acid has a loss of the carbonyl group at 500-550 K.

Benzenesulphonamide (Compound 1) is a carbonic anhydrase inhibitor. Benzenesulphonamide exhibits CA II inhibitory activity. Benzenesulphonamide reduces ROS and improves the gene expression of amyloid-β40 and 42. Benzenesulphonamide is beneficial for Alzheimer's disease. Benzenesulphonamide derivatives have anticancer, anti-inflammatory, and anticonvulsant activities. Benzenesulphonamide can be used in the research of Alzheimer's disease, epilepsy, inflammatory diseases, leukemia, melanoma, lung cancer, and colon cancer.

5,6-Dihydro-2H-pyran-2-one (Compound 1) is a prodrug-type carbonic anhydrase inhibitor. 5,6-Dihydro-2H-pyran-2-one can specifically inhibit the tumor-associated subtype hCA IX and the cytoplasmic subtype hCA I with K_i values of 1.35 and 8.03 μM. 5,6-Dihydro-2H-pyran-2-one can be used for the research on hypoxia-related cancer.

Carzenide (4-Sulfamoylbenzoic acid) is the major circulating metabolite of Mafenide (HY-B0614) in plasma. Carzenide is a strong CAII competitive inhibitor. Carzenide can be used in the research of epilepsy and cervical cancer.

Xipamide is an orally active carbonic anhydrase (CA) inhibitor and Na⁺/Cl^--potassium transporter inhibitor with diuretic and antihypertensive effects. Xipamide reduces NaCl reabsorption by inhibiting the Cl^-/NaCO₃^- anion exchanger, and increases calcium reabsorption while promoting potassium and magnesium excretion. Xipamide is mainly cleared via the renal pathway and causes a temporary decrease in glomerular filtration rate under specific conditions. Xipamide does not affect Ca²⁺ signaling induced by endothelin-1 and other factors, nor does it inhibit various ion cotransport or pump activities in red blood cells. Xipamide can be used in researches related to cardiovascular diseases, hypertension (especially with left ventricular hypertrophy), advanced renal failure, and liver cirrhosis with ascites.

CL 5343 (5-Amino-1,3,4-thiadiazole-2-sulfonamide) is a selective inhibitor of carbonic anhydrase B (HCA-B) and isoforms I, II, IV, and VII. CL 5343 has a K_i of 7.9 nM for hCA II. CL 5343 acts as a CA9 ligand to achieve targeted delivery of maytansine to the cell membrane of SKRC52 renal cancer cells. CL 5343 is useful in the development of therapeutics for diseases associated with CA overactivity, such as glaucoma, epilepsy, and cancer.

Furagin (Furazidine), an analogue of Nitrofurantoin (HY-A0090), is an antibiotic with antibacterial activity against ESKAPE pathogens with MIC values of 0-32 µg/mL. Furagin inhibits human Carbonic anhydrases . Furagin is promising for research of cancer and urinary tract infections (UTIs).

Elsulfavirine (R-1206) is an orally active human carbonic anhydrase (carbonic anhydrase, CA) inhibitor and an allosteric inhibitor of HIV-1 non-nucleoside reverse transcriptase (NNRT). Elsulfavirine also targets and blocks the interaction between adenylosuccinate lyase (ADSL) and insulin-induced gene proteins INSIG1/2, blocks SREBP-1-mediated de novo lipid synthesis, and inhibits the proliferation of liver cancer cells. The combination of Elsulfavirine and Lenvatinib (HY-10981) produces a synergistic anti-tumor effect. Elsulfavirine is converted into the active metabolite VM1500A in vivo, blocks the DNA polymerase activity of reverse transcriptase, and inhibits HIV-1 replication. Elsulfavirine exhibits a K_i of 1960 nM-52400 nM against human carbonic anhydrase isoforms including I, VII, VI, VA, VB, IX, XIII, XIV. Elsulfavirine is used in studies related to HIV-1 infection and liver cancer.

Trichlormethiazide is an orally active thiazide diuretic, with antihypertensive effect. Trichlormethiazide increases urine volume (UV), Na and K excretion and tends to improve the depressed creatinine clearance (CCRE) in acute renal failure rats model.

Sultiame is a carbonic anhydrase inhibitor, widely used as an antiepileptic agent.

Dichlorphenamide (Diclofenamide) is an orally active, specific, carbonic anhydrase inhibitor. Dichlorphenamide can reduce intraocular pressure by inhibiting the secretion of water from the eye. Dichlorphenamide can be used for glaucoma research.

4-Bromo-1H-indazole is a carbonic anhydrase inhibitor, with an IC₅₀ of 0.403 mM and a K_i of 0.383 mM against hCA-I, as well as an IC₅₀ of 0.700 mM and a K_i of 0.935 mM against hCA-II. 4-Bromo-1H-indazole reduces the catalytic activity of human I and II isoforms of carbonic anhydrase.

2-Aminobenzenesulfonamide is a carbonic anhydrase IX inhibitor.

Halazone is an atypical antimicrobial sulfonamide derivative and a carbonic anhydrase II inhibitor with a K_d value of 1.45 μM. Halazone protects sodium channels from inactivation. Halazone is widely used for disinfection of drinking water.

Acetazolamide-d₃ is deuterium labeled Acetazolamide (HY-B0782). Acetazolamide is a carbonic anhydrase (CA) IX inhibitor with an IC₅₀ of 30 nM for hCA IX. Acetazolamide has diuretic, antihypertensive and anti-gonococcal activities.

2-Methoxybenzoic acid (NSC 3778; O-Methylsalicylic acid; Salicylic acid methyl ether) is a natural compound with potential salicylate-like effect. 2-Methoxybenzoic acid inhibits carbonic anhydrase activity, elevates intraplatelet cyclic guanosine monophosphate level, and suppresses cytosolic phospholipase A₂ phosphorylation. 2-Methoxybenzoic acid suppresses platelet reactivity, including decreased spreading, retraction, and aggregation in platelets. 2-Methoxybenzoic acid ameliorates arterial thrombosis in a dose-dependent manner without affecting normal hemostasis in mice. 2-Methoxybenzoic acid can be used for the research of arterial thrombosis.

4-Chloro-3-sulfamoylbenzoic acid is a weak inhibitor of human carbonic anhydrase isoforms hCA I, hCA II, hCA IV, and hCA IX, and a synthesis intermediate for carbonic anhydrase inhibitors. 4-Chloro-3-sulfamoylbenzoic acid is the major metabolite of tripamide detected in tissues, urine, and feces of rats and rabbits following Tripamide (HY-106570) administration. 4-Chloro-3-sulfamoylbenzoic acid can be used for the study of carbonic anhydrase inhibition and species differences in drug metabolism.

Lasamide is a potent human Carbonic Anhydrase inhibitor with K_i values of 7.54 and 2.76 nM for hCAXII and hCAIX, respectively.

Carbonic anhydrase inhibitor 16 (compound 1) is a dengue protease inhibitor with inhibitory activity against carbonic anhydrase hCA I and hCA II (K_i: 28.5 nM, 2.2 nM).

Enpp/Carbonic anhydrase-IN-2 (compound 1i) is a potent Enpp and carbonic anhydrase inhibitor with IC₅₀s of 1.13, 1.07, 0.74, 0.33, 0.68 for NPP1, NPP2, NPP3, CA-IX, CA-XII respectively. Enpp/Carbonic anhydrase-IN-2 shows antiproliferative activity for cancer cells and low cytotoxic against normal cells. Enpp/Carbonic anhydrase-IN-2 induces Apoptosis.