Journal ArticleDOI
Carbonic anhydrase inhibitors. Part 43. Schiff bases derived from aromatic sulfonamides: towards more specific inhibitors for membrane-bound versus cytosolic isozymes
Claudiu T. Supuran,and Andrea Scozzafava,A Popescu,R. Bobes‐Tureac,A Banciu,A. Creanga,G. Bobes‐Tureac,Banciu +7 more
TLDR
Several new compounds showed a modest two-fold selectivity for the membrane-bound (bovine) isozyme, CA IV (bCA IV) as compared to the cytosolic human isozymes hCA I and II, in contrast to classical inhibitors which are 17–33 times less effective against bCA IV.About:
This article is published in European Journal of Medicinal Chemistry.The article was published on 1997-05-01. It has received 52 citations till now. The article focuses on the topics: Carbonic anhydrase & Isozyme.read more
Citations
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PatentDOI
Carbonic anhydrase inhibitors
Peter Ebbesen,Claudlu T. Supuran,Andrea Scozzafava,Erik Olai Pettersen,Kaye Williams,L.J. Dubois,Philippe Lambin +6 more
TL;DR: A carbonic anhydrase IX (CA IX) inhibitor is a compound of general formula: R-NH-CX-NH-(CH 2 ) n -Ar-Q-SO 2 -NH 2 or a pharmaceutically acceptable salt, derivative or prodrug thereof.
Journal ArticleDOI
Carbonic anhydrases as targets for medicinal chemistry
TL;DR: Several important physiological and physio-pathological functions are played by CAs present in organisms all over the phylogenetic tree, related to respiration and transport of carbon dioxide to bicarbonate between metabolizing tissues and the lungs, pH and CO(2) homeostasis, electrolyte secretion in a variety of tissues/organs, biosynthetic reactions, such as the gluconeogenesis and ureagenesis among others.
Journal ArticleDOI
Carbonic anhydrase inhibitors: synthesis of water-soluble, topically effective intraocular pressure lowering aromatic/heterocyclic sulfonamides containing 8-quinoline-sulfonyl moieties: is the tail more important than the ring?
Joaquín Borrás,Andrea Scozzafava,Luca Menabuoni,Francesco Mincione,Fabrizio Briganti,Giovanna Mincione,Claudiu T. Supuran +6 more
TL;DR: It is proved that the tail conferring water solubility to a sulfonamide CA inhibitor is more important for its topical activity as antiglaucoma drug than the heterocyclic/aromatic ring to which the sulfonamido moiety is grafted.
Journal ArticleDOI
Carbonic anhydrase inhibitors — Part 52. Metal complexes of heterocyclic sulfonamides: A new class of strong topical intraocular pressure-lowering agents in rabbits
Claudiu T. Supuran,Francesco Mincione,Andrea Scozzafava,Fabrizio Briganti,Giovanna Mincione,Marc A. Ilies +5 more
TL;DR: A new sulfonamide possessing strong carbonic anhydrase (CA) inhibitory properties has been prepared by reaction of 5-amino-1,3,4-thiadiazole-2-sulfonamide with adamantyl-1-carboxylic acid chloride as mentioned in this paper.
Journal ArticleDOI
Carbonic anhydrase inhibitors. Inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, IX, and XII with Schiff’s bases incorporating chromone and aromatic sulfonamide moieties, and their zinc complexes
Luca Puccetti,Giuseppe Fasolis,Daniela Vullo,Zahid H. Chohan,Andrea Scozzafava,Claudiu T. Supuran +5 more
TL;DR: Some of these compounds may show applications for the development of therapies targeting hypoxic tumors in which CA IX and XII are often highly overexpressed, and for the simple, benzenesulfonamide derivatives activity increased with an increase of the spacer from sulfanilamide to homosulf anilamide and 4-aminoethylbenzenes sulfuronamide derivative, respectively.
References
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Journal ArticleDOI
The catalytic mechanism of carbonic anhydrase: implications of a rate-limiting protolysis of water
David N. Silverman,Sven Lindskog +1 more
Journal ArticleDOI
Structure of native and apo carbonic anhydrase II and structure of some of its anion-ligand complexes.
TL;DR: A reaction scheme where electrophilic activation of carbon dioxide plays an important role in the hydration reaction is presented and the protonized oxygen of the bicarbonate is forced upon the zinc ion, thereby facilitating cleavage of the carbon-oxygen bond.
Journal ArticleDOI
The carbonic anhydrases: widening perspectives on their evolution, expression and function.
TL;DR: Now, some 55 years after its discovery in bovine red cells, carbonic anhydrase (CA), in all its varied forms, continues to challenge and intrigue physiologists, biochemists and molecular geneticists.
Journal ArticleDOI
Sulphanilamide as a Specific Inhibitor of Carbonic Anhydrase
Thaddeus Mann,D. Keilin +1 more
TL;DR: This enzyme plays an important part in accelerating the carbon dioxide output in the lungs; it appears also to promote the formation of hydrochloric acid by the parietal cells of gastric mucosa.