N
Nicola Micale
Researcher at University of Messina
Publications - 109
Citations - 2560
Nicola Micale is an academic researcher from University of Messina. The author has contributed to research in topics: Chemistry & AMPA receptor. The author has an hindex of 26, co-authored 97 publications receiving 2133 citations. Previous affiliations of Nicola Micale include Emory University & University of Milan.
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Journal ArticleDOI
Synthesis and anticonvulsant activity of novel and potent 6,7-methylenedioxyphthalazin-1(2H)-ones.
Silvana Grasso,G.B. De Sarro,A. De Sarro,Nicola Micale,Maria Zappalà,G Puja,Baraldi M,C. De Micheli +7 more
TL;DR: The synthesis of a series of novel substituted 4-aryl-6,7-methylenedioxyphthalazin-1(2H)-ones, which shows a longer lasting anticonvulsant activity against audiogenic seizures and antagonizes in vivo seizures induced by 2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA) and kainate (KA).
Journal ArticleDOI
Development of Peptidomimetics with a Vinyl Sulfone Warhead as Irreversible Falcipain-2 Inhibitors
Roberta Ettari,Emanuela Nizi,Maria Emilia Di Francesco,Marie-Adrienne Dude,Gabriele Pradel,Radim Vicik,Tanja Schirmeister,Nicola Micale,Silvana Grasso,Maria Zappalà +9 more
TL;DR: A new class of peptidomimetic cysteine protease inhibitors based on a 1,4-benzodiazepine scaffold and on an electrophilic vinyl sulfone moiety is described, proven to be potent and selective inhibitors of falcipain-2, a cysteined protease isolated from Plasmodiumfalciparum, displaying antiplasmodial activity.
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Subunit-specific agonist activity at NR2A-, NR2B-, NR2C-, and NR2D-containing N-methyl-D-aspartate glutamate receptors
Kevin Erreger,Matthew T. Geballe,Anders S. Kristensen,Philip E. Chen,Kasper B. Hansen,C. Justin Lee,Hongjie Yuan,Phuong Le,Polina Lyuboslavsky,Nicola Micale,Lars N. Jorgensen,Rasmus P. Clausen,David J. A. Wyllie,James P. Snyder,Stephen F. Traynelis +14 more
TL;DR: Despite high homology and conserved atomic contact residues within the agonist binding pocket of NR2A and NR2D, glutamate adopts a different binding orientation that could be exploited for the development of subunit selective agonists and competitive antagonists.
Journal ArticleDOI
Falcipain-2 inhibitors
TL;DR: This review is focused on inhibitors ofFalcipain‐2, a cysteine protease from P. falciparum, which represents one of the most promising targets for antimalarial drug design.
Journal ArticleDOI
Inhibition of rhodesain as a novel therapeutic modality for human African trypanosomiasis.
Roberta Ettari,Lucia Tamborini,Ilenia C. Angelo,Nicola Micale,Andrea Pinto,Carlo De Micheli,Paola Conti +6 more
TL;DR: The main classes of rhodesain inhibitors are discussed, including peptidic, peptidomimetic, and nonpeptidic structures, emphasizing those that have exhibited an optimal match between enzymatic affinity and trypanocidal profile and those for which preclinical investigations are currently in progress.