Alessio Nocentini
University of Florence
SelectivityIsozymeDocking (molecular)Inhibitory postsynaptic potentialMolecular modelEnzymeChemistryStructure–activity relationshipIn vitroCombinatorial chemistryTransmembrane proteinIn silicoCarbonic anhydraseMoietyAcetazolamideCarbonic anhydrase IISulfonamideActive siteGene isoformBiochemistryStereochemistryCell culturePharmacologyCytosol
165Publications
26H-index
2,048Citations
Publications 167
Newest
#1Claudiu T. Supuran (UniFI: University of Florence)H-Index: 152
#2Alessio Nocentini (UniFI: University of Florence)H-Index: 26
Last. Mikhail Krasavin (SPbU: Saint Petersburg State University)H-Index: 24
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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 4.2.1.1) 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...
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#1Alessio Nocentini (UniFI: University of Florence)H-Index: 26
#2Doretta Cuffaro (UniPi: University of Pisa)H-Index: 5
Last. Claudiu T. Supuran (UniFI: University of Florence)H-Index: 152
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The synthesis and carbonic anhydrase (CA; EC 4.2.1.1) 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...
2 CitationsSource
#1Diaaeldin M. Elimam (University of Bradford)
#2Abdullah A. Elgazar (Kafrelsheikh University)H-Index: 4
Last. Wagdy M. Eldehna (Kafrelsheikh University)H-Index: 25
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Abstract null null The natural product piperine, the major bioactive alkaloid present in black pepper fruits, has the ability to modulate the functional activity of several biological targets. In this study, we have utilized the natural piperine as a tail moiety to develop new SLC-0111 analogues (6a-d, 8 and 9) as potential carbonic anhydrase inhibitors. Thereafter, different functionalities, free carboxylic acid (11a-c), acetyl (13a) and ethyl ester (13b-c), were exploited as bioisosteres of th...
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#1Dmitry Dar'in (SPbU: Saint Petersburg State University)H-Index: 14
#2Grigory Kantin (SPbU: Saint Petersburg State University)H-Index: 7
Last. Mikhail Krasavin (SPbU: Saint Petersburg State University)H-Index: 24
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#1Dmitry Dar'in (SPbU: Saint Petersburg State University)H-Index: 14
#2Grigory Kantin (SPbU: Saint Petersburg State University)H-Index: 7
Last. Mikhail Krasavin (SPbU: Saint Petersburg State University)H-Index: 24
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ABSTRACT null null Herein we report the synthesis of a set of seventeen 3-sulfonamide substituted coumarin derivatives. Prepared compounds were tested in vitro for inhibition of four physiologically relevant isoforms of the metalloenzyme human carbonic anhydrase (hCA, EC 4.2.1.1). Several coumarin sulfonamides displayed low nanomolar KI values against therapeutically relevant hCA II, IX, and XII, whereas they did not potently inhibit hCA I. Some of these compounds exerted a concentration-depende...
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#1Ilaria Dettori (UniFI: University of Florence)H-Index: 7
#2Irene Fusco (UniFI: University of Florence)H-Index: 5
Last. Felicita Pedata (UniFI: University of Florence)H-Index: 56
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Ischaemic stroke is a leading cause of death and disability. One of the major pathogenic mechanisms after ischaemia includes the switch to the glycolytic pathway, leading to tissue acidification. Carbonic anhydrase (CA) contributes to pH regulation. A new generation of CA inhibitors, AN11-740 and AN6-277 and the reference compound acetazolamide (ACTZ) were investigated in two models of brain ischaemia: in rat hippocampal acute slices exposed to severe oxygen, glucose deprivation (OGD) and in an ...
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#1Alessio Nocentini (UniFI: University of Florence)H-Index: 26
#2Chad S. Hewitt (Purdue University)H-Index: 1
Last. Claudiu T. Supuran (UniFI: University of Florence)H-Index: 152
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The bacterial pathogen Neisseria gonorrhoeae encodes for an α-class carbonic anhydrase (CA, EC 4.2.1.1), NgCA, which was investigated for its inhibition with a series of inorganic and organic anions. Perchlorate and hexafluorophosphate did not significantly inhibit NgCA CO2 hydrase activity, whereas the halides, azide, bicarbonate, carbonate, stannate, perosmate, diphosphate, divanadate, perruthenate, and trifluoromethanesulfonate showed inhibition constants in the range of 1.3-9.6 mM. Anions/sm...
1 CitationsSource
#1Francesco MincioneH-Index: 23
#2Alessio Nocentini (UniFI: University of Florence)H-Index: 26
Last. Claudiu T. Supuran (UniFI: University of Florence)H-Index: 152
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INTRODUCTION Glaucoma, a neuropathy characterized by increased intraocular pressure (IOP), is the major cause of blindness worldwide and its treatment aims at reducing IOP. AREAS COVERED The authors review the design of the main classes of anti-glaucoma agents. Drugs which interfere with the aqueous humor secretion (adrenergic agonists/antagonists, carbonic anhydrase inhibitors) and with its outflow, by means of both conventional and non-conventional pathways (prostaglandin (PG) analogs, rho kin...
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The approved drugs that target carbonic anhydrases (CA, EC 4.2.1.1), a family of zinc metalloenzymes, comprise almost exclusively of primary sulfonamides (R-SO2NH2) as the zinc binding chemotype. New clinical applications for CA inhibitors, particularly for hard-to-treat cancers, has driven a growing interest in the development of novel CA inhibitors. We recently discovered that the thiazolidinedione heterocycle, where the ring nitrogen carries no substituent, is a new zinc binding group and an ...
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#2Giulia CantiniH-Index: 17
Last. Michaela LuconiH-Index: 60
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