geoscience.net logo
+ Resolve Article
+ Follow Us
Follow on FacebookFollow on Facebook
Follow on TwitterFollow on Twitter

+ Translate
+ Subscribe to Site Feed
GeoScience Most Shared ContentMost Shared Content

Carbonic anhydrase inhibitors. Part 60. The topical intraocular pressure-lowering properties of metal complexes of a heterocyclic sulfonamide: Influence of the metal ion upon biological activity


, : Carbonic anhydrase inhibitors. Part 60. The topical intraocular pressure-lowering properties of metal complexes of a heterocyclic sulfonamide: Influence of the metal ion upon biological activity. European Journal of Medicinal Chemistry 34(7-8): 585-595, July-Aug

Metal complexes of a sulfonamide possessing strong carbonic anhydrase (CA) inhibitory properties have been obtained from the sodium salt of the sulfonamide or from the free sulfonamide in the presence of ammonia, and the following metal ions: Mg(II); Zn(II); Mn(II); Cu(II); Co(II); Ni(II); Be(II); Cd(II); Pb(II); Al(III); Fe(III) and La(III). The original sulfonamide, 5-(3,4-dichlorophenylureido)-1,3,4-thiadiazole-2-sulfonamide and its complexes were assayed for in vitro inhibition of three CA isozymes, CA I, II and IV, some of which play a critical role in ocular fluid secretion. All these compounds (the sulfonamide and its metal complexes) behave as very powerful inhibitors against the three investigated CA isozymes. The parent sulfonamide possesses strong topical pressure lowering effects in rabbits when applied as a 1% solution directly into the eye, but some of its metal complexes, such as the Mg(II); Zn(II); Mn(II) and Cu(II) derivatives, lower intraocular pressure (IOP) in exper imental animals much better. Ex vivo data showed a 98.5-99.9% inhibition of CA II and IV in ocular fluids and tissues of the rabbits treated with these agents, proving that the IOP lowering properties are due to CA inhibition. The influence of the different metal ions upon the efficiency of the obtained complexes as pressure lowering drugs are discussed, considering the possibility to design in this way more selective pharmacological agents from this class.

US$19.90

DOI: 10.1016/s0223-5234(00)80028-8


Other references

Anonymous, 1981: Integrated early childhood education: preparation for social development. Summary report and conclusions. This booklet offers an outline of the topics which were covered at the Second Eastern Hemisphere Seminar in March 1981, by presenting conclusions under four headings: (1) Early childhood education: the community dimension. (2) Integrated education...

Wilken-Jensen, C.; Pedersen, B.L., 1998: Obstetrics and the null-hypothesis. Ugeskrift for Laeger 159(50): 7509-7510

Burastero, S.E.; Mistrello, G.; Falagiani, P.; Paolucci, C.; Breda, D.; Roncarolo, D.; Zanotta, S.; Monasterolo, G.; Rossi, R.E., 2008: Effect of sublingual immunotherapy with grass monomeric allergoid on allergen-specific T-cell proliferation and interleukin 10 production. The diagnostic value of enzyme immunoassay systems manufactured by different companies was comparatively studied to detect specific IgM antibodies to measles virus. The assay systems were shown to have a high sensitivity. The specificity was highe...

Azemoto, N.; Kumagi, T.; Abe, M.; Konishi, I.; Matsuura, B.; Hiasa, Y.; Onji, M., 2011: Biochemical response to ursodeoxycholic acid predicts long-term outcome in Japanese patients with primary biliary cirrhosis. Hepatology Research 41(4): 310-317

Novik V.I.; Agroskin L.S.; Solov'eva L.V., 1989: Cytomorphologic and morphometric characteristics of endocervical epithelial malignancies. Cyto-histological and biometric analysis identified certain cytomorphological features of reserve cell hyperplasia, dysplasia (atypical hyperplasia of reserve cells), reserve cell carcinoma in situ and adenocarcinoma in situ in the cervical canal....

Howell J.A.; Velicangil O.; L.M.S.; Zeppelin A.L.H., 1981: Ultra filtration of protein solutions. Constantinides A , W R Vieth And K Venkatasubramanian (Ed ) Annals Of The New York Academy Of Sciences, Vol 369 Biochemical Engineering Ii; 2nd Biochemical Engineering Conference on Advances in Biochemical Engineering, Henniker, N H , Usa, July, 1980 Vii+384p New York Academy Of Sciences: New York, N Y , Usa Illus P355-366

Harvey, A.R.; Hellström, M.; Rodger, J., 2009: Gene therapy and transplantation in the retinofugal pathway. The mature CNS has limited intrinsic capacity for repair after injury; therefore, strategies are needed to enhance the viability and regrowth of damaged neurons. Here we review gene therapy studies in the eye, aimed at improving the survival and r...

Wang, B-Nan.; Liu, G-Qiang.; Kong, D-Yang.; Lu, J-He., 2014: Chlorination of ethynyl estradiol: a kinetic and mechanistic study. The objective of this research is to explore the fundamentals of reactions between chlorine and ethynyl estradiol (EE2), which is expected to occur during the drinking water treatment. The first step of EE2 chlorination was shown to follow the sec...

Labato, M.I.; Contrini, Mía.M.; Lazzarini, D.; Campos, A.M.; Gauna, Mía.L.; Claros, R.; López, E.L.; Savy, V.L.; Luna, C.M., 2015: Pandemic influenza A/H1N1 2009 antibodies in the metropolitan area of Buenos Aires in Argentina. To estimate the infection prevalence in Buenos Aires during the outbreak of pandemic influenza A/H1N1 2009 virus (A(H1N1)pdm09). A(H1N1)pdm09-specific antibodies were measured by hemagglutination inhibition assay in human serum samples collected 6...

Pearce, C.A.; Hyde, K.D., 1993: The genus Ophiodothella from Australia. Two species of Ophiodothella parasitic on leaves are reported from Australia. 0. longispora Swart from leaves of Eucalyptus goniocalyx is redescribed, while O. syzygii is described as new. Both species are illustrated with differential interferenc...