Claudiu T. Supuran
University of Florence
IsozymeEnzymeChemistryStructure–activity relationshipIn vitroCarbonic anhydraseMoietyEnzyme inhibitorAcetazolamideCarbonic anhydrase IISulfonamideSulfonamide (medicine)Carbonic Anhydrase IActive siteGene isoformBiochemistryStereochemistryBiologyPharmacologyCytosol
Publications 1,977
#1Ozlem Akgul (Ege University)H-Index: 5
#2Elena Lucarini (UniFI: University of Florence)H-Index: 10
Last. Claudiu T. Supuran (UniFI: University of Florence)H-Index: 155
view all 11 authors...
Abstract null null We report a series of compounds 1–17 derived from the antiepileptic drug Sulthiame (SLT) from which both the benzenesulfonamide and the sultam moiety were retained. All compounds were tested in vitro for their inhibition activity against the human (h) Carbonic Anhydrase (CA; EC I, II, VII, IX and XII isoforms. Among the series, derivatives 1 and 11 showed great enhancement of both inhibition potency and selectivity towards the hCA VII isoform, when compared to the ref...
#1Andrea Petreni (UniFI: University of Florence)H-Index: 3
#2Sameh M. Osman (KSU: King Saud University)H-Index: 21
Last. Claudiu T. Supuran (UniFI: University of Florence)H-Index: 155
view all 6 authors...
Abstract null null The first structural analysis comparing the binding mode to the target carbonic anhydrases (CAs, EC of two opposite classes of modulators is presented here: coumarin derivatives act as prodrug CA inhibitors (CAIs), being hydrolyzed by the enzyme esterase activity to 2-hydroxycinnamic acids that occlude the active site entrance; CA activators (CAAs) belonging of the amine and amino acid types, enhance the CA activity by increasing the efficiency of the rate-determining...
#1Damiano Tanini (UniFI: University of Florence)H-Index: 19
#2Simone Carradori (University of Chieti-Pescara)H-Index: 46
Last. Elena Lucarini (UniFI: University of Florence)H-Index: 10
view all 13 authors...
Abstract null null Platinum-based chemotherapy is widely used for the treatment of different tumors but is associated with serious side effects, among which neuropathic pain. Carbonic anhydrase (CA, EC inhibitors have recently been validated as therapeutic agents in neuropathic pain and as antitumor agents. We report the synthesis of new organochalcogenides bearing the benzensulfonamide moiety acting as potent inhibitors of several human CA isoforms and, in particular, against hCA II an...
#1Secil Deniz (Pamukkale University)H-Index: 3
#2Tuğba Kevser Uysal (Yıldırım Beyazıt University)H-Index: 2
Last. Ozen Ozensoy Guler (Yıldırım Beyazıt University)H-Index: 9
view all 5 authors...
The ongoing Covid-19 is a contagious disease, and it is characterised by different symptoms such as fever, cough, and shortness of breath. Rising concerns about Covid-19 have severely affected the healthcare system in all countries as the Covid-19 outbreak has developed at a rapid rate all around the globe. Intriguing, a clinically used drug, acetazolamide (a specific inhibitor of carbonic anhydrase, CA, EC, is used to treat high-altitude pulmonary oedema (HAPE), showing a high degree o...
#1Linda J. Urbański (UTA: University of Tampere)H-Index: 3
#2Daniela Vullo (UniFI: University of Florence)H-Index: 69
Last. Claudiu T. Supuran (UniFI: University of Florence)H-Index: 155
view all 4 authors...
Pathogenic bacteria resistant to most antibiotics, including the methicillin-resistant Staphylococcus aureus (MRSA) represent a serious medical problem. The search for new antiinfectives, possessing a diverse mechanism of action compared to the clinically used antibiotics, has become an attractive research field. S. aureus DNA encodes a β-class carbonic anhydrase, SauBCA. It is a druggable target that can be inhibited by certain aromatic and heterocyclic sulphonamides. Here we investigated inorg...
#1Emma Baglini (UniPi: University of Pisa)H-Index: 4
#2Rahul Ravichandran (Seconda Università degli Studi di Napoli)H-Index: 1
Last. Claudiu T. Supuran (UniFI: University of Florence)H-Index: 155
view all 12 authors...
A library of variously decorated N-phenyl secondary sulphonamides featuring the bicyclic tetrahydroquinazole scaffold was synthesised and biologically evaluated for their inhibitory activity against human carbonic anhydrase (hCA) I, II, IV, and IX. Of note, several compounds were identified showing submicromolar potency and excellent selectivity for the tumour-related hCA IX isoform. Structure-activity relationship data attained for various substitutions were rationalised by molecular modelling ...
#1Alessio Nocentini (UniFI: University of Florence)H-Index: 29
#2Claudiu T. Supuran (UniFI: University of Florence)H-Index: 155
Last. Clemente CapassoH-Index: 57
view all 3 authors...
Carbonic anhydrases (CAs, EC have been studied for decades and have been classified as a superfamily of enzymes which includes, up to date, eight gene families or classes indicated with the Greek letters α, β, γ, δ, ζ, η, θ, ι. This versatile enzyme superfamily is involved in multiple physiological processes, catalysing a fundamental reaction for all living organisms, the reversible hydration of carbon dioxide to bicarbonate and a proton. Recently, the ι-CA (LCIP63) from the diatom Thal...
#1Alessio Nocentini (UniFI: University of Florence)H-Index: 29
#2Doretta Cuffaro (UniPi: University of Pisa)H-Index: 6
Last. Claudiu T. Supuran (UniFI: University of Florence)H-Index: 155
view all 8 authors...
The synthesis and carbonic anhydrase (CA; EC activating effects of a series of oxime ether-based amino alcohols towards four human (h) CA isoforms expressed in human brain, hCA I, II, IV a...
#1Claudiu T. Supuran (UniFI: University of Florence)H-Index: 155
#2Alessio Nocentini (UniFI: University of Florence)H-Index: 29
Last. Mikhail Krasavin (SPbU: Saint Petersburg State University)H-Index: 25
view all 6 authors...
The non-nucleoside reverse transcriptase inhibitor VM1500A is approved for the treatment of HIV/AIDS in its N-acyl sulphonamide prodrug form elsulfavirine (Elpida®). Biochemical profiling against twelve human carbonic anhydrase (CA, EC isoforms showed that while elsulfavirine was a weak inhibitor of all isoforms, VM1500A potently and selectively inhibited human (h) hCA VII isoform, a proven target for the therapy of neuropathic pain. The latter is a common neurologic complication of HIV...
Abstract null null Carbonic anhydrase IX is a promising target for the search for new antitumor compounds with improved properties. Using the molecular hybridization approach, on the basis of structures of a selective carbonic anhydrase IX inhibitor 3 and an activator of apoptosis 2 (1), a series of 1-substituted isatin-5-sulfonamides 5a–5u were designed and synthesized. The study of the inhibitory activity of isatin-5-sulfonamides showed the ability to inhibit I, II, IX, XII isoforms at nano- a...
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