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.

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 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.

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