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

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.

1996 ◽  
Vol 3 (2) ◽  
pp. 79-83 ◽  
Author(s):  
Claudiu T. Supuran

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).


1998 ◽  
Vol 5 (1) ◽  
pp. 11-18 ◽  
Author(s):  
Andrea Scozzafava ◽  
Christine Cavazza ◽  
Claudiu T. Supuran ◽  
Ioana Saramet ◽  
Fabrizio Briganti ◽  
...  

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.


1996 ◽  
Vol 3 (3) ◽  
pp. 143-148 ◽  
Author(s):  
Joaquin Borràs ◽  
Javier Casanova ◽  
Teodora Cristea ◽  
Adriana Gheorghe ◽  
Andrea Scozzafava ◽  
...  

Ternary Ni(II) complexes of hydrazine and eight heterocyclic sulfonamides possessing carbonic anhydrase (CA) inhibitory properties, were prepared and characterized by elemental analysis, spectroscopic, magnetic, thermogravimetric, and conductimetric measurements. The complexes behave as strong inhibitors for two isozymes (I and II) of carbonic anhydrase.


1997 ◽  
Vol 4 (1) ◽  
pp. 19-26 ◽  
Author(s):  
Andrea Scozzafava ◽  
Claudiu T. Supuran

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.


1997 ◽  
Vol 4 (1) ◽  
pp. 1-7 ◽  
Author(s):  
Andrei Jitianu ◽  
Marc A. llies ◽  
Fabrizio Briganti ◽  
Andrea Scozzafava ◽  
Claudiu T. Supuran

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.


2002 ◽  
Vol 339 ◽  
pp. 532-542 ◽  
Author(s):  
Jean Michel Grevy ◽  
Fabiola Tellez ◽  
Sylvain Bernés ◽  
Heinrich Nöth ◽  
Rosalinda Contreras ◽  
...  

Author(s):  
N. N. Malyutina ◽  
A. F. Bolotova ◽  
R. B. Eremeev ◽  
A. Zh. Gilmanov ◽  
D. Yu. Sosnin

Introduction. The overwhelming number of publications contains only data on the content of individual antioxidants, but not on the overall antioxidant activity of the blood in patients with vibration disease.The aim of the study was to determine the total antioxidant activity of blood serum in patients with vibration disease.Materials and methods. Th e main group consisted of 30 people diagnosed with “Vibration disease” of 1 degree (n=21) and 2 degrees (n=9). Th e control group consisted of 30 clinically healthy men, comparable in age with the main group (p=0.66). Th e total activity of antioxidant systems of blood plasma was evaluated photometrically using the test system “Total antioxidant status-Novo” (“Vector-best”, Russia).Results. The indicator of the total antioxidant status (TAS) was 1,038±0.232 mmol/l in the examined main group, against 1,456±0.225 mmol/l in the examined control group (p<0.000001). Th e coefficient of variation (CV) in patients with vibration disease was 22.35%, 1.45 times higher than in the control group (15.45%). In the main group there was a positive correlation between age and TAS (R=0.525), in the control group there was no such relationship (R=0.095). Th e degree of decrease depended on the severity of vibration disease.Conclusions. 1. The development of vibration disease is accompanied by a decrease in the antioxidant status of blood serum. 2. Th e degree of decrease in the antioxidant status of blood serum correlates with the severity of vibration disease. 3. Reduction of TAS can serve as a pathogenetic justification of the need to include drugs and/or biologically active additives with antioxidant activity in therapy


Author(s):  
A. V. Kadomtsevа ◽  
I. V. Zhdanovich ◽  
M. S. Piskunovа ◽  
A. N. Lineva ◽  
A. N. Novikova ◽  
...  

The synthesis of biologically active coordination compounds and the design on their basis of effective pharmacological preparations is currently the promising area. This paper presents the results of the toxicological studies on digermanium and its complex derivatives. It should be noted that the positive medical properties of organometallic compounds of germanium are confirmed by numerous studies, therefore, the development of the methods of synthesis, as well as investigations of physicochemical and pharmacological properties of these compounds are at the center of attention.


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