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 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 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 Again about carbonic anhydrase inhibitors: modern aspects of the use of ICA in ophthalmology

2021 ◽  
Vol 9 (2) ◽  
pp. 64-71
Author(s):  
P.A. Bezdetko
Keyword(s):  
Antioxidant Activity ◽  
Intraocular Pressure ◽  
Optic Nerve ◽  
Carbonic Anhydrase ◽  
Macular Edema ◽  
Mechanism Of Action ◽  
Corneal Endothelium ◽  
Complex Treatment ◽  
Efficacy And Safety ◽  
Carbonic Anhydrase Inhibitors

For more than 70 years, the inhibitors of carbonic anhydrase (ICA) have been used in the treatment of glaucoma. Since 1995, topical forms of ICA have appeared among antiglaucoma drugs — dorzolamide, and since 1999 — brinzolamide. The hypotensive efficacy and safety of topical ICA gave rise to the widespread use of these drugs in the treatment of various forms of glaucoma. The peculiarities of the mechanism of action made it possible to create on their basis effective fixed combinations, which allow reducing the intraocular pressure by up to 40 % in patients with glaucoma. The attractiveness of the drug has expanded due to the effect of ICA on various tissues of the organ of vision. Thus, ICAs effectively improve the hemodynamics of the eye and optic nerve. The antioxidant activity of the drug makes it possible to expand the indications for its use in patients with vascular patho-logy of the retina and optic nerve. The biomechanical characte-ristics of the drug allowed its effective and safe use in the complex treatment of macular edema of various etiologies. The adjuvant use of topical ICAs expands the possibilities of anti-VEGF therapy in the treatment of macular edema of various etiologies. Features of the action of ICA on the endothelial pump function of the cornea made it possible to formulate the rules for the use of topical ICA in patients with an insufficient function of the corneal endothelium.

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