Search

Your search keyword '"Consalvi, Sara"' showing total 4 results
Start Over Author "Consalvi, Sara" Topic nitric oxide
4 results on '"Consalvi, Sara"'

1. Therapeutic potential for coxibs-nitric oxide releasing hybrids in cystic fibrosis.

Author

Consalvi S, Poce G, Ghelardini C, Di Cesare Mannelli L, Patrignani P, Bruno A, Anzini M, Calderone V, Martelli A, Testai L, Giordani A, and Biava M

Subjects
Animals, Anti-Inflammatory Agents, Non-Steroidal chemistry, Cyclooxygenase 2 metabolism, Cyclooxygenase 2 Inhibitors chemistry, Cystic Fibrosis metabolism, Humans, Inflammation drug therapy, Inflammation metabolism, Molecular Structure, Nitric Oxide chemistry, Anti-Inflammatory Agents, Non-Steroidal pharmacology, Cyclooxygenase 2 Inhibitors pharmacology, Cystic Fibrosis drug therapy, Nitric Oxide pharmacology
Abstract

This review discusses the rational for further studies of COX-2 inhibitors-NO releaser hybrids (NO-Coxibs) in the pharmacological treatment of the airway inflammation in Cystic Fibrosis (CF). Our research group developed several classes of NO-Coxibs for the pharmacological treatment of arthritis, and among them several compounds showed an outstanding in vivo efficacy and good pharmacokinetic properties. The good antiinflammatory properties displayed by these compounds during the previous screening could, by itself, suggest appropriate candidates for further testing in CF., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2020 Elsevier Masson SAS. All rights reserved.)

Published
2021
Full Text
View/download PDF

2. A Series of COX-2 Inhibitors Endowed with NO-Releasing Properties: Synthesis, Biological Evaluation, and Docking Analysis.

Author

Consalvi S, Poce G, Ragno R, Sabatino M, La Motta C, Sartini S, Calderone V, Martelli A, Ghelardini C, Di Cesare Mannelli L, and Biava M

Subjects
Cyclooxygenase 2 Inhibitors chemistry, Dose-Response Relationship, Drug, Humans, Molecular Structure, Nitric Oxide Donors chemical synthesis, Structure-Activity Relationship, Cyclooxygenase 2 metabolism, Cyclooxygenase 2 Inhibitors chemical synthesis, Cyclooxygenase 2 Inhibitors pharmacology, Molecular Docking Simulation, Nitric Oxide metabolism, Nitric Oxide Donors chemistry, Nitric Oxide Donors pharmacology
Abstract

Herein we report the synthesis, biological evaluation, and docking analysis of a class of cyclooxygenase-2 (COX-2) inhibitors with nitric oxide (NO)-releasing properties. In an earlier study, a number of selective COX-2 inhibitors/NO donors were developed by conjugating a diarylpyrrole scaffold endowed with selective COX-2 inhibitory properties with various nitrooxyalkyl side chains such as esters, α-amino esters, amides, α-amino amides, ethers, β-amino ethers, inverse esters, and amides. These candidates were found to have high in vitro potencies (COX-2 inhibition at 10 μm: ≥96 %), great efficacy in determining NO-vasorelaxing responses, and good antinociceptive activity in an abdominal writhing test. Among the compounds synthesized in the present work, derivative 2 b [2-(2-(1-(3-fluorophenyl)-2-methyl-5-(4-sulfamoylphenyl)-1H-pyrrol-3-yl)acetamido)ethyl nitrate] showed particularly outstanding activity, with efficacy similar to that of celecoxib even at very low concentrations., (© 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)

Published
2016
Full Text
View/download PDF

3. Enhancing the pharmacodynamic profile of a class of selective COX-2 inhibiting nitric oxide donors.

Author

Biava M, Battilocchio C, Poce G, Alfonso S, Consalvi S, Di Capua A, Calderone V, Martelli A, Testai L, Sautebin L, Rossi A, Ghelardini C, Di Cesare Mannelli L, Giordani A, Persiani S, Colovic M, Dovizio M, Patrignani P, and Anzini M

Subjects
Acetic Acid, Amides chemistry, Animals, Carrageenan, Cell Line, Constriction, Pathologic chemically induced, Constriction, Pathologic drug therapy, Cyclooxygenase 2 Inhibitors chemistry, Edema chemically induced, Edema drug therapy, Glycine analogs & derivatives, Glycine chemistry, Humans, Hyperalgesia chemically induced, Hyperalgesia drug therapy, Liver metabolism, Male, Mice, Nitrates metabolism, Nitrites metabolism, Rats, Rats, Wistar, Structure-Activity Relationship, Amides pharmacology, Cyclooxygenase 2 metabolism, Cyclooxygenase 2 Inhibitors pharmacology, Glycine pharmacology, Nitric Oxide chemistry
Abstract

We report herein the development, synthesis, physicochemical and pharmacological characterization of a novel class of pharmacodynamic hybrids that selectively inhibit cyclooxygenase-2 (COX-2) isoform and present suitable nitric oxide releasing properties. The replacement of the ester moiety with the amide group gave access to in vivo more stable and active derivatives that highlighted outstanding pharmacological properties. In particular, the glycine derivative proved to be extremely active in suppressing hyperalgesia and edema., (Copyright © 2013 Elsevier Ltd. All rights reserved.)

Published
2014
Full Text
View/download PDF

4. Improving the solubility of a new class of antiinflammatory pharmacodynamic hybrids, that release nitric oxide and inhibit cycloxygenase-2 isoenzyme.

Author

Biava M, Battilocchio C, Poce G, Alfonso S, Consalvi S, Porretta GC, Schenone S, Calderone V, Martelli A, Testai L, Ghelardini C, Di Cesare Mannelli L, Sautebin L, Rossi A, Giordani A, Patrignani P, and Anzini M

Subjects
Acetic Acid, Animals, Anti-Inflammatory Agents, Non-Steroidal chemistry, Anti-Inflammatory Agents, Non-Steroidal pharmacokinetics, Carrageenan antagonists & inhibitors, Carrageenan pharmacology, Constriction, Pathologic chemically induced, Dose-Response Relationship, Drug, Enzyme Inhibitors pharmacokinetics, Isoenzymes antagonists & inhibitors, Isoenzymes metabolism, Male, Mice, Molecular Structure, Muscle, Smooth, Vascular chemistry, Muscle, Smooth, Vascular drug effects, Muscle, Smooth, Vascular metabolism, Rats, Rats, Sprague-Dawley, Rats, Wistar, Solubility, Structure-Activity Relationship, Anti-Inflammatory Agents, Non-Steroidal pharmacology, Constriction, Pathologic drug therapy, Cyclooxygenase 2 metabolism, Enzyme Inhibitors chemistry, Enzyme Inhibitors pharmacology, Nitric Oxide metabolism
Abstract

The development of a novel class of pharmacodynamic hybrids that inhibits COX-2 isoform is reported. These molecules display enhanced nitric oxide releasing properties due to the presence of an ionisable moiety. The in vivo analgesic/anti-inflammatory activity was maintained in relation to the parent compounds., (Copyright © 2012 Elsevier Masson SAS. All rights reserved.)

Published
2012
Full Text
View/download PDF

Catalog

Books, media, physical & digital resources
See catalog results