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Author Andrea Angeli

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Heterologous expression and biochemical characterisation of the recombinant β-carbonic anhydrase (MpaCA) from the warm-blooded vertebrate pathogen malassezia pachydermatis.

Viviana De Luca, Andrea Angeli, Valeria Mazzone, Claudia Adelfio, Vincenzo Carginale, Andrea Scaloni, Fabrizio Carta, Silvia Selleri, Claudiu T Supuran, Clemente Capasso,

Warm-blooded animals may have Malassezia pachydermatis on healthy skin, but changes in the skin microenvironment or host defences induce this opportunistic commensal to become pathogenic. Malassezia infections in humans and animals are commonly treated with azole antifungals. Fungistatic treatments, together with their long-term use, contribute to the selection and the ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2022, 37(1):62-68]

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One-Pot Procedure for the Synthesis of Asymmetric Substituted Ureido Benzene Sulfonamides as Effective Inhibitors of Carbonic Anhydrase Enzymes.

Gioele Vannozzi, Daniela Vullo, Andrea Angeli, Marta Ferraroni, Jacob Combs, Carrie Lomelino, Jacob Andring, Robert Mckenna, Gianluca Bartolucci, Marco Pallecchi, Laura Lucarini, Silvia Sgambellone, Emanuela Masini, Fabrizio Carta, Claudiu T Supuran,

We report a one-pot procedure for the synthesis of asymmetrical ureido-containing benzenesulfonamides based on in situ generation of the corresponding isocyanatobenezenesulfonamide species, which were trapped with the appropriate amines. A library of new compounds was generated and evaluated in vitro for their inhibition properties against a representative panel of the ... Read more >>

J Med Chem (Journal of medicinal chemistry)
[2022, 65(1):824-837]

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Calixarenes Incorporating Sulfonamide Moieties: Versatile Ligands for Carbonic Anhydrases Inhibition.

Davide Sbravati, Alessandro Bonardi, Silvia Bua, Andrea Angeli, Marta Ferraroni, Marta Ferraroni, Alessio Nocentini, Alessandro Casnati, Paola Gratteri, Francesco Sansone, Claudiu T Supuran,

Carbonic anhydrases (CAs) continue to represent a relevant pharmaceutical target. The need of selective inhibitors and the involvement of these metalloenzymes in many multifaceted diseases boost the search for new ligands able to distinguish among the different CA isoforms, and for multifunctional systems simultaneously able to inhibit CAs and to ... Read more >>

Chemistry (Chemistry (Weinheim an der Bergstrasse, Germany))
[2021, :e202103527]

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Ureidosulfocoumarin Derivatives As Selective and Potent Carbonic Anhydrase IX and XII Inhibitors.

Priti Singh, Dilep Kumar Sigalapalli, Nerella Sridhar Goud, Baijayantimala Swain, Santosh Kumar Sahoo, Andrea Angeli, Afzal B Shaik, Venkata Madhavi Yaddanapudi, Claudiu T Supuran, Mohammed Arifuddin,

Owing to severe allergic reactions (anaphylaxis) and resistance exhibited by sulfonamide-based carbonic anhydrase (CA) inhibitors, non-classical or non-sulfonamide CA inhibitors are gaining increased attention by medicinal chemists. In this context, we report the design and synthesis of 30 new non-sulfonamide sulfocoumarin derivatives as CA inhibitors. They were investigated against hCA ... Read more >>

ChemMedChem (ChemMedChem)
[2021, :e202100725]

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Activation of the β-carbonic anhydrase from the protozoan pathogen Trichomonas vaginalis with amines and amino acids.

Andrea Angeli, Linda J Urbański, Vesa P Hytönen, Seppo Parkkila, Claudiu T Supuran,

We report the first activation study of the β-class carbonic anhydrase (CA, EC 4.2.1.1) encoded in the genome of the protozoan pathogen <i>Trichomonas vaginalis</i>, TvaCA1. Among 24 amino acid and amine activators investigated, derivatives incorporating a second carboxylic moiety, such as L-Asp, L- and D-Glu, were devoid of activating effects ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2021, 36(1):758-763]

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Reconsidering anion inhibitors in the general context of drug design studies of modulators of activity of the classical enzyme carbonic anhydrase.

Alessio Nocentini, Andrea Angeli, Fabrizio Carta, Jean-Yves Winum, Raivis Zalubovskis, Simone Carradori, Clemente Capasso, William A Donald, Claudiu T Supuran,

Inorganic anions inhibit the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1) generally by coordinating to the active site metal ion. Cyanate was reported as a non-coordinating CA inhibitor but those erroneous results were subsequently corrected by another group. We review the anion CA inhibitors (CAIs) in the more general context of ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2021, 36(1):561-580]

Cited: 16 times

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Carbonic anhydrase activation profile of indole-based derivatives.

Elisabetta Barresi, Rahul Ravichandran, Lorenzo Germelli, Andrea Angeli, Emma Baglini, Silvia Salerno, Anna Maria Marini, Barbara Costa, Eleonora Da Pozzo, Claudia Martini, Federico Da Settimo, Claudiu Supuran, Sandro Cosconati, Sabrina Taliani,

Carbonic Anhydrase Activators (CAAs) could represent a novel approach for the treatment of Alzheimer's disease, ageing, and other conditions that require remedial achievement of spatial learning and memory therapy. Within a research project aimed at developing novel CAAs selective for certain isoforms, three series of indole-based derivatives were investigated. Enzyme ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2021, 36(1):1783-1797]

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Selective inhibition of carbonic anhydrase IX and XII by coumarin and psoralen derivatives.

Rita Meleddu, Serenella Deplano, Elias Maccioni, Francesco Ortuso, Filippo Cottiglia, Daniela Secci, Alessia Onali, Erica Sanna, Andrea Angeli, Rossella Angius, Stefano Alcaro, Claudiu T Supuran, Simona Distinto,

A small library of coumarin and their psoralen analogues <b>EMAC10157a-b-d-g</b> and <b>EMAC10160a-b-d-g</b> has been designed and synthesised to investigate the effect of structural modifications on their inhibition ability and selectivity profile towards carbonic anhydrase isoforms I, II, IX, and XII. None of the new compounds exhibited activity towards hCA I ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2021, 36(1):685-692]

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Inhibition of the β-carbonic anhydrase from the protozoan pathogen Trichomonas vaginalis with sulphonamides.

Linda J Urbański, Andrea Angeli, Vesa P Hytönen, Anna Di Fiore, Giuseppina De Simone, Seppo Parkkila, Claudiu T Supuran,

Sulphonamides and their isosteres are classical inhibitors of the carbonic anhydrase (CAs, EC 4.2.1.1) metalloenzymes. The protozoan pathogen <i>Trichomonas vaginalis</i> encodes two such enzymes belonging to the β-class, TvaCA1 and TvaCA2. Here we report the first sulphonamide inhibition study of TvaCA1, with a series of simple aromatic/heterocyclic primary sulphonamides as ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2021, 36(1):329-334]

Cited: 2 times

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2-(2-Hydroxyethyl)piperazine derivatives as potent human carbonic anhydrase inhibitors: Synthesis, enzyme inhibition, computational studies and antiglaucoma activity.

Niccolò Chiaramonte, Andrea Angeli, Silvia Sgambellone, Alessandro Bonardi, Alessio Nocentini, Gianluca Bartolucci, Laura Braconi, Silvia Dei, Laura Lucarini, Elisabetta Teodori, Paola Gratteri, Bernhard Wünsch, Claudiu T Supuran, Maria Novella Romanelli,

Targeting Carbonic Anhydrases (CAs) represents a strategy to treat several diseases, from glaucoma to cancer. To widen the structure-activity relationships (SARs) of our series of piperazines endowed with potent human carbonic anhydrase (hCA) inhibition, a new series of chiral piperazines carrying a (2-hydroxyethyl) group was prepared. The Zn-binding function, the ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2022, 228:114026]

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Amine- and Amino Acid-Based Compounds as Carbonic Anhydrase Activators.

Andrea Angeli, Emanuela Berrino, Simone Carradori, Claudiu T Supuran, Marzia Cirri, Fabrizio Carta, Gabriele Costantino,

After being rather neglected as a research field in the past, carbonic anhydrase activators (CAAs) were undoubtedly demonstrated to be useful in diverse pharmaceutical and industrial applications. They also improved the knowledge of the requirements to selectively interact with a CA isoform over the others and confirmed the catalytic mechanism ... Read more >>

Molecules (Molecules (Basel, Switzerland))
[2021, 26(23):]

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Carbonic Anhydrase Inhibition with Sulfonamides Incorporating Pyrazole- and Pyridazinecarboxamide Moieties Provides Examples of Isoform-Selective Inhibitors.

Andrea Angeli, Victor Kartsev, Anthi Petrou, Mariana Pinteala, Volodymyr Brovarets, Roman Vydzhak, Svitlana Panchishin, Athina Geronikaki, Claudiu T Supuran,

A series of benzenesulfonamides incorporating pyrazole- and pyridazinecarboxamides decorated with several bulky moieties has been obtained by original procedures. The new derivatives were investigated for the inhibition of four physiologically crucial human carbonic anhydrase (hCA, EC 4.2.2.1.1) isoforms, hCA I and II (cytosolic enzymes) as well as hCA IX and ... Read more >>

Molecules (Molecules (Basel, Switzerland))
[2021, 26(22):]

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Inhibitory Effects of Sulfonamide Derivatives on the β-Carbonic Anhydrase (MpaCA) from Malassezia pachydermatis, a Commensal, Pathogenic Fungus Present in Domestic Animals.

Viviana De Luca, Andrea Angeli, Valeria Mazzone, Claudia Adelfio, Fabrizio Carta, Silvia Selleri, Vincenzo Carginale, Andrea Scaloni, Claudiu T Supuran, Clemente Capasso,

Fungi are exposed to various environmental variables during their life cycle, including changes in CO<sub>2</sub> concentration. CO<sub>2</sub> has the potential to act as an activator of several cell signaling pathways. In fungi, the sensing of CO<sub>2</sub> triggers cell differentiation and the biosynthesis of proteins involved in the metabolism and pathogenicity ... Read more >>

Int J Mol Sci (International journal of molecular sciences)
[2021, 22(22):]

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Ex Vivo Fecal Fermentation of Human Ileal Fluid Collected After Wild Strawberry Consumption Modulates Human Microbiome Community Structure and Metabolic Output and Protects Against DNA Damage in Colonic Epithelial Cells.

Camilla Diotallevi, Massimiliano Fontana, Cheryl Latimer, Nigel G Ternan, L Kirsty Pourshahidi, Roger Lawther, Gloria O'Connor, Lorenza Conterno, Mattia Gasperotti, Andrea Angeli, Cesare Lotti, Martina Bianchi, Urska Vrhovsek, Francesca Fava, Marco Gobbetti, Chris I R Gill, Kieran M Tuohy,

<h4>Scope</h4>Wild strawberries (Fragaria vesca) are richer in (poly)phenols than common commercial strawberry varieties, e.g., Fragaria × ananassa. (Poly)phenols and their microbiota-derived metabolites are hypothesized to exert bioactivity within the human gut mucosa. To address this, the effects of wild strawberries are investigated with respect to their bioactivity and microbiota-modulating capacity ... Read more >>

Mol Nutr Food Res (Molecular nutrition & food research)
[2021, :e2100405]

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Selective Inhibition of Helicobacter pylori Carbonic Anhydrases by Carvacrol and Thymol Could Impair Biofilm Production and the Release of Outer Membrane Vesicles.

Rossella Grande, Simone Carradori, Valentina Puca, Irene Vitale, Andrea Angeli, Alessio Nocentini, Alessandro Bonardi, Paola Gratteri, Paola Lanuti, Giuseppina Bologna, Pasquale Simeone, Clemente Capasso, Viviana De Luca, Claudiu T Supuran,

<i>Helicobacter pylori</i>, a Gram-negative neutrophilic pathogen, is the cause of chronic gastritis, peptic ulcers, and gastric cancer in humans. Current therapeutic regimens suffer from an emerging bacterial resistance rate and poor patience compliance. To improve the discovery of compounds targeting bacterial alternative enzymes or essential pathways such as carbonic anhydrases ... Read more >>

Int J Mol Sci (International journal of molecular sciences)
[2021, 22(21):]

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Glyco-Coated CdSe/ZnS Quantum Dots as Nanoprobes for Carbonic Anhydrase IX Imaging in Cancer Cells.

Giacomo Biagiotti, Andrea Angeli, Arianna Giacomini, Gianluca Toniolo, Luca Landini, Gianluca Salerno, Lorenzo Di Cesare Mannelli, Carla Ghelardini, Tommaso Mello, Silvia Mussi, Cosetta Ravelli, Marcello Marelli, Stefano Cicchi, Enzo Menna, Roberto Ronca, Claudiu T Supuran, Barbara Richichi,

The bioimaging of cancer cells by the specific targeting of overexpressed biomarkers is an approach that holds great promise in the identification of selective diagnostic tools. Tumor-associated human carbonic anhydrase (hCA) isoforms IX and XII have been considered so far as well-defined biomarkers, with their expression correlating with cancer progression ... Read more >>

ACS Appl Nano Mater (ACS applied nano materials)
[2021, 4(12):14153-14160]

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Sultam based Carbonic Anhydrase VII inhibitors for the management of neuropathic pain.

Özlem Akgül, Elena Lucarini, Lorenzo Di Cesare Mannelli, Carla Ghelardini, Katia D'Ambrosio, Martina Buonanno, Simona Maria Monti, Giuseppina De Simone, Andrea Angeli, Claudiu T Supuran, Fabrizio Carta,

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 4.2.1.1) I, II, VII, IX and XII isoforms. ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2022, 227:113956]

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Biochemical and structural characterization of beta-carbonic anhydrase from the parasite Trichomonas vaginalis.

Linda J Urbański, Andrea Angeli, Vasyl V Mykuliak, Latifeh Azizi, Marianne Kuuslahti, Vesa P Hytönen, Claudiu T Supuran, Seppo Parkkila,

Trichomonas vaginalis is a unicellular parasite and responsible for one of the most common sexually transmittable infections worldwide, trichomoniasis. Carbonic anhydrases (CAs) are enzymes found in all lifeforms and are known to play a vital role in many biochemical processes in organisms including the maintenance of acid-base homeostasis. To date, ... Read more >>

J Mol Med (Berl) (Journal of molecular medicine (Berlin, Germany))
[2022, 100(1):115-124]

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Novel benzenesulfonamide-bearing pyrazoles and 1,2,4-thiadiazoles as selective carbonic anhydrase inhibitors.

Rajiv Kumar, Amit Kumar, Sita Ram, Andrea Angeli, Alessandro Bonardi, Alessio Nocentini, Paola Gratteri, Claudiu T Supuran, Pawan K Sharma,

Two series comprising 20 novel benzenesulfonamides bearing thioureido-linked pyrazole 8 and amino-1,2,4-thiadiazole 10 were synthesized and assayed as human carbonic anhydrase (hCA) inhibitors against isoforms I and II as well as the tumor-associated isoforms IX and XII. Molecular modeling studies of some potent derivatives (8a, 8c, 10a, and 10c) were ... Read more >>

Arch Pharm (Weinheim) (Archiv der Pharmazie)
[2022, 355(1):e2100241]

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Design and development of novel series of indole-3-sulfonamide ureido derivatives as selective carbonic anhydrase II inhibitors.

Priti Singh, Abhishek Choli, Baijayantimala Swain, Andrea Angeli, Santosh K Sahoo, Venkata M Yaddanapudi, Claudiu T Supuran, Mohammed Arifuddin,

Indole is a privileged moiety with a wide range of bioactivities, making it a popular scaffold in drug design and development studies as well as in synthetic chemistry. Here, novel urea derivatives of indole, containing sulfonamide at position-3 of indole, were synthesized using a well-known tail approach, as carbonic anhydrases ... Read more >>

Arch Pharm (Weinheim) (Archiv der Pharmazie)
[2022, 355(1):e2100333]

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4-Sulfamoylphenylalkylamides as Inhibitors of Carbonic Anhydrases Expressed in Vibrio cholerae.

Francesca Mancuso, Laura De Luca, Federica Bucolo, Milan Vrabel, Andrea Angeli, Clemente Capasso, Claudiu T Supuran, Rosaria Gitto,

A current issue of antimicrobial therapy is the resistance to treatment with worldwide consequences. Thus, the identification of innovative targets is an intriguing challenge in the drug and development process aimed at newer antimicrobial agents. The state-of-art of anticholera therapy might comprise the reduction of the expression of cholera toxin, ... Read more >>

ChemMedChem (ChemMedChem)
[2021, 16(24):3787-3794]

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New Sulfanilamide Derivatives Incorporating Heterocyclic Carboxamide Moieties as Carbonic Anhydrase Inhibitors.

Andrea Angeli, Victor Kartsev, Anthi Petrou, Mariana Pinteala, Roman M Vydzhak, Svitlana Y Panchishin, Volodymyr Brovarets, Viviana De Luca, Clemente Capasso, Athina Geronikaki, Claudiu T Supuran,

Carbonic Anhydrases (CAs) are ubiquitous metalloenzymes involved in several disease conditions. There are 15 human CA (hCA) isoforms and their high homology represents a challenge for the discovery of potential drugs devoid of off-target side effects. For this reason, many synthetic and pharmacologic research efforts are underway to achieve the ... Read more >>

Pharmaceuticals (Basel) (Pharmaceuticals (Basel, Switzerland))
[2021, 14(8):]

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Chalcogenides-incorporating carbonic anhydrase inhibitors concomitantly reverted oxaliplatin-induced neuropathy and enhanced antiproliferative action.

Damiano Tanini, Simone Carradori, Antonella Capperucci, Lucrezia Lupori, Susi Zara, Marta Ferraroni, Carla Ghelardini, Ldc Mannelli, Laura Micheli, Elena Lucarini, Fabrizio Carta, Andrea Angeli, Claudiu T Supuran,

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 4.2.1.1) inhibitors have recently been validated as therapeutic agents in neuropathic pain and as antitumor agents. We report the synthesis of new organochalcogenides bearing ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2021, 225:113793]

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Mechanisms of the Antiproliferative and Antitumor Activity of Novel Telomerase-Carbonic Anhydrase Dual-Hybrid Inhibitors.

Anna A Plyasova, Emanuela Berrino, Irina I Khan, Alexander V Veselovsky, Vadim S Pokrovsky, Andrea Angeli, Marta Ferraroni, Claudiu T Supuran, Marina V Pokrovskaya, Svetlana S Alexandrova, Yulia A Gladilina, Nikolay N Sokolov, Abdullah Hilal, Fabrizio Carta, Dmitry D Zhdanov,

Human (h) telomerase (TL; EC 2.7.7.49) plays a key role in sustaining cancer cells by means of elongating telomeric repeats at the 3' ends of chromosomes. Since TL-inhibitor (TI) stand-alone cancer therapy has been proven to be remarkably challenging, a polypharmacological approach represents a valid alternative. Here we consider a ... Read more >>

J Med Chem (Journal of medicinal chemistry)
[2021, 64(15):11432-11444]

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Selenolesterase enzyme activity of carbonic anhydrases.

Andrea Angeli, Fabrizio Carta, Selene Donnini, Antonella Capperucci, Marta Ferraroni, Damiano Tanini, Claudiu T Supuran,

Carbonic anhydrases (CAs, E.C. 4.2.1.1) are metalloenzymes expressed on a variety of cell types. Their overexpression leads to serious pathologies, including cancer. The discovery of a series of selenolesters with high structural diversity as novel CA inhibitors is reported here. These compounds show remarkable in vitro inhibition against a panel ... Read more >>

Chem Commun (Camb) (Chemical communications (Cambridge, England))
[2020, 56(32):4444-4447]

Cited: 1 time

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