scholarly journals Complexes With Biologically Active Ligands. Part 111. Synthesis and Carbonic Anhydrase Inhibitory Activity of Metal Complexes of 4,5-Disubstituted-3-Mercapto-1,2,4-Triazole Derivatives

1998 ◽  
Vol 5 (1) ◽  
pp. 11-18 ◽  
Author(s):  
Andrea Scozzafava ◽  
Christine Cavazza ◽  
Claudiu T. Supuran ◽  
Ioana Saramet ◽  
Fabrizio Briganti ◽  
...  
Keyword(s):  
Intraocular Pressure ◽  
Nmr Spectroscopy ◽  
Animal Models ◽  
Carbonic Anhydrase ◽  
Metal Ions ◽  
Metal Complexes ◽  
Elemental Analysis ◽  
Inhibitory Activity ◽  
Biologically Active ◽  
Standard Procedures

Complexes containing five 4,5-disubstituted-3-mercapto-1,2,4-triazoles and Zn(II), Hg(II) and Cu(I) were synthesized and characterized by standard procedures (elemental analysis; IR, electronic and NMR spectroscopy, conductimetry and TG analysis). Both the thione as well as the thiolate forms of the ligands were evidenced to interact with the metal ions in the prepared complexes. The original mercaptans and their metal complexes behave as inhibitors of three carbonic anhydrase (CA) isozymes, CA I, II and IV, but did not lower intraocular pressure in rabbits in animal models of glaucoma.

scholarly journals Complexes With Biologically Active Ligands. Part 101 Inhibition of Carbonic Anhydrase Isozymes I and II With Metal Complexes of Imidazo[2,1−b]-1,3,4-Thiadiazole-2-Sulfonamide

1997 ◽  
Vol 4 (1) ◽  
pp. 19-26 ◽  
Author(s):  
Andrea Scozzafava ◽  
Claudiu T. Supuran
Keyword(s):  
Carbonic Anhydrase ◽  
Metal Ions ◽  
Metal Complexes ◽  
Elemental Analysis ◽  
Epr Spectroscopy ◽  
Title Compound ◽  
Biologically Active ◽  
Standard Procedures

The title compound was prepared by an improved variant of the literature procedure, and metal complexes containing its anion and the following metal ions: Zn(II), Cd(II), Hg(II), Co(II), Ni(II), Cu(II), V(IV), Fe(III) and Ag(I) were synthesized and characterized by standard procedures (elemental analysis; IR, electronic, NMR and EPR spectroscopy; TG, magnetic and conductimetric measurements). The parent sulfonamide and its metal complexes are potent inhibitors of two carbonic anhydrase (CA) isozymes, CA I and II, and they might possess applications as selective cerebrovasodilating agents.

scholarly journals Complexes With Biologically Active Ligands. Part 91 Metal Complexes of 5-Benzoylamino- and 5-(3-Nitrobenzoyl-Amino)-1,3,4-Thiadiazole-2-Sulfonamide as Carbonic Anhydrase Inhibitors

1997 ◽  
Vol 4 (1) ◽  
pp. 1-7 ◽  
Author(s):  
Andrei Jitianu ◽  
Marc A. llies ◽  
Fabrizio Briganti ◽  
Andrea Scozzafava ◽  
Claudiu T. Supuran
Keyword(s):  
Carbonic Anhydrase ◽  
Metal Complexes ◽  
Elemental Analysis ◽  
Epr Spectroscopy ◽  
Biologically Active ◽  
Carbonic Anhydrase Inhibitors ◽  
Standard Procedures

Complexes containing the anions of 5-benzoylamido-1,3,4-thiadiazole-2-sulfonamide and 5-(3-nitro-benzoylamido)-1,3,4-thiadiazole-2-sulfonamid as ligands, and V(IV); Cr(III); Fe(III); Co(II); Ni(II); Cu(II) and Ag(I) were synthesized and characterized by standard procedures (elemental analysis; IR, electronic, and EPR spectroscopy; TG, magnetic and conductimetric measurements). The original sulfonamides and their metal complexes are strong inhibitors of two carbonic anhydrase (CA) isozymes, CA I and II.

scholarly journals Carbonic Anhydrase Inhibitors Part 721 Synthesis and Antiglaucoma Properties of Metal Complexes of p-Fluorobenzolamide

1999 ◽  
Vol 6 (2) ◽  
pp. 67-73 ◽  
Author(s):  
Claudiu T. Supuran ◽  
Andrea Scozzafava ◽  
Luca Menabuoni ◽  
Francesco Mincione ◽  
Fabrizio Briganti ◽  
...  
Keyword(s):  
Intraocular Pressure ◽  
Carbonic Anhydrase ◽  
Metal Ions ◽  
Metal Complexes ◽  
Carbonic Anhydrase Inhibitors ◽  
Physico Chemical ◽  
New Compounds

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. The new complexes contained metal ions such as Zn(II), Cu(II), Co(II), Ni(II), Cd(II) and Mn(II). The new compounds were characterized by standard physico-chemical procedures, and assayed as inhibitors of three CA isozymes, CA I, II and IV. Very good inhibition has been evidenced both for the parent sulfonamides as well as for the prepared complexes, against all three investigated isozymes. Some of these new complexes as well as the parent sulfonamide, strongly lowered intraocular pressure (IOP) in normotensive rabbits when administered as a 2% solution into the eye.

scholarly journals Complexes With Biologically Active Ligands. Part 4. Coordination Compounds of Chlorothiazide With Transition Metal Ions Behave as Strong Carbonic Anhydrase Inhibitors

1996 ◽  
Vol 3 (2) ◽  
pp. 79-83 ◽  
Author(s):  
Claudiu T. Supuran
Keyword(s):  
Transition Metal ◽  
Carbonic Anhydrase ◽  
Metal Ions ◽  
Elemental Analysis ◽  
Coordination Compounds ◽  
Transition Metal Ions ◽  
Biologically Active ◽  
Carbonic Anhydrase Inhibitors

Complexes of the diuretic benzothiadiazine derivative chlorothiazide (6-chloro-7-sulfamoyl- 1,2,4-benzothiadiazine-1,1-dioxide) with V(IV); Fe(II); Co(II); Ni(II); Cu(II), Ag(I) and U(VI) were prepared and characterized by elemental analysis, spectroscopic, thermogravimetric, magnetic and conductimetric measurements. The complexes behave as effective inhibitors for two isozymes (I and II) of carbonic anhydrase (CA).

scholarly journals Complexes With Biologically Active Ligands. Part 1. Synthesis of Coordination Compounds of Diazoxide With Transition- and Main-Group Cations

1996 ◽  
Vol 3 (1) ◽  
pp. 25-30 ◽  
Author(s):  
Claudiu T. Supuran
Keyword(s):  
Carbonic Anhydrase ◽  
Metal Ions ◽  
Elemental Analysis ◽  
Coordination Compounds ◽  
Main Group ◽  
Pharmacological Agent ◽  
Biologically Active ◽  
Modest Activity

Complexes of diazoxide (3-methyl-7-chloro-1,2,4-benzothiadiazine-1,1-dioxide) - an antihypertensive and hyperglycemic pharmacological agent - with a series of transition- and main-group di-, triand tetravalent metal ions were prepared and characterized by elemental analysis, spectroscopic, thermogravimetric, magnetic and conductimetric measurements. The complexes were tested as inhibitors of the enzyme carbonic anhydrase (CA), proving modest activity towards CA II and better inhibition of CA I.

scholarly journals Carbonic Anhydrase Inhibitors. Part 461 Inhibition of Carbonic Anhydrase Isozymes I, II and IV With Trifluoromethylsulfonamide Derivatives and Their Zinc(II) and Copper(II) Complexes

1997 ◽  
Vol 4 (1) ◽  
pp. 27-34 ◽  
Author(s):  
Giovanna Mincione ◽  
Andrea Scozzafava ◽  
Claudiu T. Supuran
Keyword(s):  
Carbonic Anhydrase ◽  
Elemental Analysis ◽  
Inhibitory Activity ◽  
Free Amino ◽  
Amino Group ◽  
Carbonic Anhydrase Inhibitors ◽  
Standard Procedures ◽  
Aromatic Heterocyclic

Reaction of aromatic/heterocyclic sulfonamides containing a free amino group with triflic anhydride afforded compounds possessing trifluoromethanesulfonamido moieties in their molecule. The Zn(II) and Cu(II) complexes of these new sulfonamides were prepared and characterized by standard procedures (elemental analysis, spectroscopic, magnetic, thermogravimetric and conductimetric measurements). The new derivatives showed good inhibitory activity against three isozymes of carbonic anhydrase (CA), i.e., CA I, II and IV.

scholarly journals Carbonic Anhydrase Inhibitors. Part 541: Metal Complexes of Heterocyclic Sulfonamides: A New Class of Antiglaucoma Agents

1997 ◽  
Vol 4 (6) ◽  
pp. 307-315 ◽  
Author(s):  
Claudiu T. Supuran ◽  
Andrea Scozzafava ◽  
Andrei Jitianu
Keyword(s):  
Intraocular Pressure ◽  
Carbonic Anhydrase ◽  
Metal Ions ◽  
Metal Complexes ◽  
Carbonic Anhydrase Inhibitors ◽  
Experimental Animals ◽  
New Class ◽  
Physico Chemical ◽  
Main Group Metal ◽  
Antiglaucoma Agents

Metal complexes of heterocyclic sulfonamides possessing carbonic anhydrase (CA) inhibitory properties were recently shown to be useful as intraocular pressure (IOP) lowering agents in experimental animals, and might be developed as a novel class of antiglaucoma drugs. Here we report the synthesis of a heterocyclic sulfonamide CA inhibitor and of the metal complexes containing main group metal ions, such as Be(II), Mg(II), Al(III), Zn(II), Cd(II) and Hg(II) and the new sulfonamide as well as 5-amino-1,3,4-thiadiazole-2-sulfonamide as ligands. The new complexes were characterized by standard physico-chemical procedures, and assayed as inhibitors of three CA isozymes, CA I, II and IV. Some of them (but not the parent sulfonamides) strongly lowered IOP in rabbits when administered as a 2% solution into the eye.

Studies on complexes of VO(II), Mn(II), Cu(II), Ni(II), Co(II), Zn(II), Fe(III), and UO2(II) with hydrazone β-diketone ligands

1990 ◽  
Vol 68 (5) ◽  
pp. 774-781 ◽  
Author(s):  
Mohamed S. Abdel-Moez ◽  
Shaker L. Stefan ◽  
Mostafa M. El-Behairy ◽  
Mohamed M. Mashely ◽  
Basheir A. El-Shetary
Keyword(s):  
Magnetic Susceptibility ◽  
Transition Metal ◽  
Ir Spectra ◽  
Metal Ions ◽  
Metal Complexes ◽  
Stability Constants ◽  
Transition Metal Complexes ◽  
Elemental Analysis ◽  
Water Solvent ◽  
Uv Visible

The stepwise stability constants of VO(II), Mn(II), Cu(II), Ni (II), Co(II), Zn(II), Fe(III), and UO2(II) metal ions with 2-(2-acetylphenylhydrazone)-5,5-dimethyl-1,3-cyclohexane dione (2-APHDm), 3-(2-acetylphenylhydrazone)pentane-2,4-dione (2-APHA), 2-(2-acetylphenylhydrazone)-1-phenyl-1,3-butane dione (2-APHB), 2-(2-acetylphenylhydrazone)-1,3-diphenyl-1,3-propane dione (2-APHDB), and 3-(2-acetylphenylhydrazone)-1,1,1-trifluoropentane-2,4-dione (2-APHTA) were determined at 30 °C by pH titrations in 75% (v/v) dioxane–water solvent. In addition, metal complexes of three related β-diketones, 2-APHA, 2-APHB, and 2-APHDB have been synthesized and characterized by elemental analysis, uv–visible, ir spectra, and conductance in DMF and magnetic susceptibility measurements. The structure of the complexes have been proposed. Keywords: transition metal complexes of hydrazone-β-diketone ligands.

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