scholarly journals Metal Complexes of 1,3,4-Thiadiazole-2,5-Disulfonamide are Strong Dual Carbonic Anhydrase Inhibitors, although the Ligand Possesses very Weak such Properties

1995 ◽  
Vol 2 (6) ◽  
pp. 331-336 ◽  
Author(s):  
Claudiu T. Supuran
Keyword(s):  
Carbonic Anhydrase ◽  
Metal Complexes ◽  
Coordination Compounds ◽  
Uv Spectroscopy ◽  
Carbonic Anhydrase Inhibitors ◽  
Strong Dual ◽  
Ir And Uv Spectroscopy ◽  
Parent Ligand

Coordination compounds of Co(II), Ni(II), Cu(II), Zn(II), and Cd(II) with 1,3,4-thiadiazole-2,5-disulfonamide as ligand were synthesized and characterized by IR and UV spectroscopy, conductimetry and thermogravimetry. The parent ligand is a very weak carbonic anhydrase (CA) inhibitor, although it constituted the lead for developing important classes of diuretics. The complex derivatives behave as much stronger CA inhibitors, with IC50 values around 10−8 M against isozyme CA II, and 10−7 M against isozyme CAI.

scholarly journals Carbonic Anhydrase Inhibitors. Part 551 Metal Complexes of 1,3,4-Thiadiazole-2-Sulfonamide Derivatives: In Vitro Inhibition Studies With Carbonic Anhydrase Isozymes I, II and IV

1998 ◽  
Vol 5 (2) ◽  
pp. 103-114 ◽  
Author(s):  
Claudiu T. Supuran ◽  
Andrea Scozzafava ◽  
Fabrizio Briganti ◽  
Marc A. Ilies ◽  
Andrei Jitianu
Keyword(s):  
Carbonic Anhydrase ◽  
Metal Complexes ◽  
Coordination Compounds ◽  
Active Sites ◽  
Carbonic Anhydrase Inhibitors ◽  
Standard Procedures ◽  
In Vitro Inhibition ◽  
Characteristic Features ◽  
Inhibition Studies

Coordination compounds of 5-chloroacetamido-1,3,4-thiadiazole-2-sulfonamide (Hcaz) with V(IV), Cr(lll), Fe(ll), Co(ll), Ni(ll) and Cu(ll) have been prepared and characterized by standard procedures (spectroscopic, magnetic, EPR, thermogravimetric and conductimetric measurements). Some of these compounds showed very good in vitro inhibitory properties against three physiologically relevant carbonic anhydrase (CA)isozymes, i.e., CA I, II, and IV. The differences between these isozymes in susceptibility to inhibition by these metal complexes is discussed in relationship to the characteristic features of their active sites, and is rationalized in terms useful for developing isozyme-specific CA inhibitors.

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.

Metal Complexes of Heterocyclic Sulfonamides as Carbonic Anhydrase Inhibitors

2010 ◽  
Author(s):  
Joaquín Borrás ◽  
Gloria Alzuet ◽  
Sacramento Ferrer ◽  
Claudiu T Supuran
Keyword(s):  
Carbonic Anhydrase ◽  
Metal Complexes ◽  
Carbonic Anhydrase Inhibitors

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).

Metal Complexes of Heterocyclic Sulfonamides as Carbonic Anhydrase Inhibitors

2004 ◽  
pp. 183-207
Author(s):  
Sacramento Ferrer ◽  
Gloria Alzuet ◽  
Claudiu Supuran ◽  
Joaquín Borrás
Keyword(s):  
Carbonic Anhydrase ◽  
Metal Complexes ◽  
Carbonic Anhydrase Inhibitors

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.

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