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Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with phosphates, carbamoyl phosphate, and the phosphonate antiviral drug foscarnet.
Rusconi S, Innocenti A, Vullo D, Mastrolorenzo A, Scozzafava A, Supuran CT. Rusconi S, et al. Bioorg Med Chem Lett. 2004 Dec 6;14(23):5763-7. doi: 10.1016/j.bmcl.2004.09.064. Bioorg Med Chem Lett. 2004. PMID: 15501037
The cytosolic isozyme hCA II was weakly inhibited by all the investigated anions, with carbamoyl phosphate showing a K(I) of 0.31 mM. ...The mitochondrial isozyme hCA V was weakly inhibited by all phosphates/phosphonates, except carbamoyl phosphate, which showed a K …
The cytosolic isozyme hCA II was weakly inhibited by all the investigated anions, with carbamoyl phosphate showing a K(I) of 0.31 mM. …
Carbonic Anhydrase Inhibitors Part 72 Synthesis and Antiglaucoma Properties of Metal Complexes of p-Fluorobenzolamide.
Supuran CT, Scozzafava A, Menabuoni L, Mincione F, Briganti F, Mincione G. Supuran CT, et al. Met Based Drugs. 1999;6(2):67-73. doi: 10.1155/MBD.1999.67. Met Based Drugs. 1999. PMID: 18475883 Free PMC article.
Metal complexes of a heterocyclic sulfonamides possessing very strong carbonic anhydrase (CA) inhibitory properties, i.e., 5-(p-fluorobenzenesulfonylamido)-1,3,4-thiadiazole-2-sulfonamide (p-fluorobenzolamide) were prepared. ...Some of these new complexes as well as the pa …
Metal complexes of a heterocyclic sulfonamides possessing very strong carbonic anhydrase (CA) inhibitory properties, i.e., 5-(p-fluor …
Carbonic Anhydrase Inhibitors. Part 55 Metal Complexes of 1,3,4-Thiadiazole-2-Sulfonamide Derivatives: In Vitro Inhibition Studies With Carbonic Anhydrase Isozymes I, II and IV.
Supuran CT, Scozzafava A, Briganti F, Ilies MA, Jitianu A. Supuran CT, et al. Met Based Drugs. 1998;5(2):103-14. doi: 10.1155/MBD.1998.103. Met Based Drugs. 1998. PMID: 18475829 Free PMC article.
Complexes with biologically active ligands. Part 11. Synthesis and carbonic anhydrase inhibitory activity of metal complexes of 4,5-disubstituted-3-mercapto-1,2,4-triazole derivatives.
Scozzafava A, Cavazza C, Supuran CT, Saramet I, Briganti F, Banciu MD. Scozzafava A, et al. Met Based Drugs. 1998;5(1):11-8. doi: 10.1155/MBD.1998.11. Met Based Drugs. 1998. PMID: 18475819 Free PMC article.
Carbonic Anhydrase Activators. Part 19 Spectroscopic and Kinetic Investigations for the Interaction of Isozymes I and II With Primary Amines.
Briganti F, Scozzafava A, Supuran CT. Briganti F, et al. Met Based Drugs. 1997;4(4):221-7. doi: 10.1155/MBD.1997.221. Met Based Drugs. 1997. PMID: 18475791 Free PMC article.
This is a direct spectroscopic evidence that the activator molecules bind within the active site, but not directly to the metal ion. ...
This is a direct spectroscopic evidence that the activator molecules bind within the active site, but not directly to the metal ion. …
Carbonic anhydrase activation enhances object recognition memory in mice through phosphorylation of the extracellular signal-regulated kinase in the cortex and the hippocampus.
Canto de Souza L, Provensi G, Vullo D, Carta F, Scozzafava A, Costa A, Schmidt SD, Passani MB, Supuran CT, Blandina P. Canto de Souza L, et al. Among authors: scozzafava a. Neuropharmacology. 2017 May 15;118:148-156. doi: 10.1016/j.neuropharm.2017.03.009. Epub 2017 Mar 9. Neuropharmacology. 2017. PMID: 28286213
Anion inhibition studies of two α-carbonic anhydrases from Lotus japonicus, LjCAA1 and LjCAA2.
Vullo D, Flemetakis E, Scozzafava A, Capasso C, Supuran CT. Vullo D, et al. J Inorg Biochem. 2014 Jul;136:67-72. doi: 10.1016/j.jinorgbio.2014.03.014. Epub 2014 Apr 8. J Inorg Biochem. 2014. PMID: 24769135
LjCAA1 showed a high catalytic activity for the CO2 hydration reaction, with a k(cat) of 7.4∗10(5) s(-1) and a k(cat)/K(m) of 9.6∗10(7) M(-1) s(-1) and was inhibited in the low micromolar range by N,N-diethyldithiocarbamate, sulfamide, sulfamic acid, phenylbo …
LjCAA1 showed a high catalytic activity for the CO2 hydration reaction, with a k(cat) of 7.4∗10(5) s(-1) and a k(cat)/K …
7-Substituted-sulfocoumarins are isoform-selective, potent carbonic anhydrase II inhibitors.
Tanc M, Carta F, Bozdag M, Scozzafava A, Supuran CT. Tanc M, et al. Bioorg Med Chem. 2013 Aug 1;21(15):4502-10. doi: 10.1016/j.bmc.2013.05.032. Epub 2013 May 31. Bioorg Med Chem. 2013. PMID: 23769167
A series of 7-substituted sulfocoumarins and 3,4-dihydrosulfocoumarins was obtained by cyclization of the methanesulfonate of 2,4-dihydroxy- or 2-hydroxy-4-methoxybenzaldehyde, followed by derivatization reactions. The new compounds incorporate a range of substituen
A series of 7-substituted sulfocoumarins and 3,4-dihydrosulfocoumarins was obtained by cyclization of the methanesulfonate of 2,4-dih
Discovery of low nanomolar and subnanomolar inhibitors of the mycobacterial beta-carbonic anhydrases Rv1284 and Rv3273.
Güzel O, Maresca A, Scozzafava A, Salman A, Balaban AT, Supuran CT. Güzel O, et al. J Med Chem. 2009 Jul 9;52(13):4063-7. doi: 10.1021/jm9004016. J Med Chem. 2009. PMID: 19438226
A series of 2-(hydrazinocarbonyl)-3-aryl-1H-indole-5-sulfonamides has been derivatized by reaction with 2,4,6-trimethylpyrylium perchlorate, leading to pyridinium derivatives. ...
A series of 2-(hydrazinocarbonyl)-3-aryl-1H-indole-5-sulfonamides has been derivatized by reaction with 2,4,6-trimethylpyrylium perch
Carbonic anhydrase inhibitors: aliphatic N-phosphorylated sulfamates--a novel zinc-anchoring group leading to nanomolar inhibitors.
Bonnac L, Innocenti A, Winum JY, Casini A, Montero JL, Scozzafava A, Barragan V, Supuran CT. Bonnac L, et al. J Enzyme Inhib Med Chem. 2004 Jun;19(3):275-8. doi: 10.1080/14756360410001689522. J Enzyme Inhib Med Chem. 2004. PMID: 15500000
A small library of phosphorylated sulfamates (N-(O-alkylsulfamoyl)-phosphoramidic acids) incorporating long aliphatic chains (C8-C16) has been synthesized and investigated for their interaction with two physiologically relevant carbonic anhydrase (CA) isozymes. ...The phos
A small library of phosphorylated sulfamates (N-(O-alkylsulfamoyl)-phosphoramidic acids) incorporating long aliphatic chains (C8-C16)
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