A
Antonio Scilimati
Researcher at University of Bari
Publications - 143
Citations - 2207
Antonio Scilimati is an academic researcher from University of Bari. The author has contributed to research in topics: Aryl & Kinetic resolution. The author has an hindex of 25, co-authored 133 publications receiving 1903 citations. Previous affiliations of Antonio Scilimati include University of Chieti-Pescara & University of Wisconsin-Madison.
Papers
More filters
Journal ArticleDOI
Selective COX-1 inhibition: A therapeutic target to be reconsidered.
TL;DR: This review would elucidate the most recent findings on selective COX-1 inhibition and their relevance to human pathology such as cancer, neuro-inflammation, cardioprotection, fever and pain, and focus on the design and development of new highly selective COx-1 inhibitors, useful tools in pharmacological studies.
Journal ArticleDOI
De Novo Synthesis of Cyclooxygenase-1 Counteracts the Suppression of Platelet Thromboxane Biosynthesis by Aspirin
Virgilio Evangelista,Stefano Manarini,Angelo Di Santo,Marta L. Capone,Emanuela Ricciotti,Luigia Di Francesco,Stefania Tacconelli,Andrea Sacchetti,Sandra D’Angelo,Antonio Scilimati,Maria G. Sciulli,Paola Patrignani +11 more
TL;DR: In washed human platelets, the complete suppression of TXA2 biosynthesis by aspirin, in vitro, recovered in response to thrombin and fibrinogen in a time-dependent fashion and was blocked by translational inhibitors, by rapamycin, and by inhibitors of phosphatidylinositol 3-kinase.
Journal ArticleDOI
Synthesis, pharmacological characterization, and docking analysis of a novel family of diarylisoxazoles as highly selective cyclooxygenase-1 (COX-1) inhibitors.
Paola Vitale,Stefania Tacconelli,Maria Grazia Perrone,Paola Malerba,Laura Simone,Antonio Scilimati,Antonio Lavecchia,Melania Dovizio,Emanuela Marcantoni,Annalisa Bruno,Paola Patrignani +10 more
TL;DR: 3g, 3s, and 3d were more potent inhibitors of platelet COX-1 and aggregation than P6 (named 6) for their tighter binding to the enzyme, and the pharmacological results were supported by docking simulations.
Journal ArticleDOI
Novel Synthesis of 3,4-Diarylisoxazole Analogues of Valdecoxib: Reversal Cyclooxygenase-2 Selectivity by Sulfonamide Group Removal
TL;DR: 3,4-Diarylisoxazole analogues of valdecoxib, a selective cyclooxygenase-2 (COX-2) inhibitor, were synthesized by 1,3-dipolar cycloaddition of arylnitrile oxides to the enolate ion of phenylacetone regioselectively prepared in situ with lithium diisopropylamide at 0 degrees C.
Journal ArticleDOI
Structural basis for selective inhibition of Cyclooxygenase-1 (COX-1) by diarylisoxazoles mofezolac and 3-(5-chlorofuran-2-yl)-5-methyl-4-phenylisoxazole (P6).
Gino Cingolani,Gino Cingolani,Andrea Panella,Maria Grazia Perrone,Paola Vitale,Giuseppe Di Mauro,Cosimo G. Fortuna,Roger S. Armen,Savina Ferorelli,William L. Smith,Antonio Scilimati +10 more
TL;DR: The structural basis for COX-1 binding to two diarylisoxazoles is determined: mofezolac, which is polar and ionizable, and 3-(5-chlorofuran-2-yl)-5-methyl-4-phenylisoxazole (P6) that has very low polarity.