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Items: 1 to 50 of 58

1.

Synthesis and Anti-HIV Profile of a Novel Tetrahydroindazolylbenzamide Derivative Obtained by Oxazolone Chemistry.

Scala A, Piperno A, Micale N, Christ F, Debyser Z.

ACS Med Chem Lett. 2018 Dec 15;10(4):398-401. doi: 10.1021/acsmedchemlett.8b00511. eCollection 2019 Apr 11.

2.

Hydroxamic Acid-Based Histone Deacetylase (HDAC) Inhibitors Bearing a Pyrazole Scaffold and a Cinnamoyl Linker.

Zagni C, Citarella A, Oussama M, Rescifina A, Maugeri A, Navarra M, Scala A, Piperno A, Micale N.

Int J Mol Sci. 2019 Feb 21;20(4). pii: E945. doi: 10.3390/ijms20040945.

3.

Discovery of benzimidazole-based Leishmania mexicana cysteine protease CPB2.8ΔCTE inhibitors as potential therapeutics for leishmaniasis.

De Luca L, Ferro S, Buemi MR, Monforte AM, Gitto R, Schirmeister T, Maes L, Rescifina A, Micale N.

Chem Biol Drug Des. 2018 Sep;92(3):1585-1596. doi: 10.1111/cbdd.13326. Epub 2018 May 31.

PMID:
29729080
4.

Antimicrobial peptide capsids of de novo design.

De Santis E, Alkassem H, Lamarre B, Faruqui N, Bella A, Noble JE, Micale N, Ray S, Burns JR, Yon AR, Hoogenboom BW, Ryadnov MG.

Nat Commun. 2017 Dec 22;8(1):2263. doi: 10.1038/s41467-017-02475-3.

5.

"Click" on PLGA-PEG and hyaluronic acid: Gaining access to anti-leishmanial pentamidine bioconjugates.

Scala A, Piperno A, Micale N, Mineo PG, Abbadessa A, Risoluti R, Castelli G, Bruno F, Vitale F, Cascio A, Grassi G.

J Biomed Mater Res B Appl Biomater. 2018 Nov;106(8):2778-2785. doi: 10.1002/jbm.b.34058. Epub 2017 Dec 8.

PMID:
29219244
6.

Ensemble-based ADME-Tox profiling and virtual screening for the discovery of new inhibitors of the Leishmania mexicana cysteine protease CPB2.8ΔCTE.

Scala A, Rescifina A, Micale N, Piperno A, Schirmeister T, Maes L, Grassi G.

Chem Biol Drug Des. 2018 Feb;91(2):597-604. doi: 10.1111/cbdd.13124. Epub 2017 Nov 10.

PMID:
29045053
7.

Physicochemical properties of inclusion complexes of highly soluble β-cyclodextrins with highly hydrophobic testosterone propionate.

Celia C, Scala A, Stancanelli R, Surdo E, Paolino D, Grattoni A, Micale N, Crupi V, Majolino D, Fresta M, Tommasini S, Venuti V, Ventura CA.

Int J Pharm. 2017 Dec 20;534(1-2):316-324. doi: 10.1016/j.ijpharm.2017.10.014. Epub 2017 Oct 16.

PMID:
29042336
8.

Gold compounds as cysteine protease inhibitors: perspectives for pharmaceutical application as antiparasitic agents.

Massai L, Messori L, Micale N, Schirmeister T, Maes L, Fregona D, Cinellu MA, Gabbiani C.

Biometals. 2017 Apr;30(2):313-320. doi: 10.1007/s10534-017-0007-0. Epub 2017 Mar 10.

PMID:
28283781
9.

Synthesis of C3/C1-Substituted Tetrahydroisoquinolines.

Mihoubi M, Micale N, Scala A, Jarraya RM, Bouaziz A, Schirmeister T, Risitano F, Piperno A, Grassi G.

Molecules. 2015 Aug 14;20(8):14902-14. doi: 10.3390/molecules200814902.

10.

Selected cytotoxic gold compounds cause significant inhibition of 20S proteasome catalytic activities.

Micale N, Schirmeister T, Ettari R, Cinellu MA, Maiore L, Serratrice M, Gabbiani C, Massai L, Messori L.

J Inorg Biochem. 2014 Dec;141:79-82. doi: 10.1016/j.jinorgbio.2014.08.001. Epub 2014 Aug 11.

PMID:
25217719
11.

Optimization of peptidomimetic boronates bearing a P3 bicyclic scaffold as proteasome inhibitors.

Troiano V, Scarbaci K, Ettari R, Micale N, Cerchia C, Pinto A, Schirmeister T, Novellino E, Grasso S, Lavecchia A, Zappalà M.

Eur J Med Chem. 2014 Aug 18;83:1-14. doi: 10.1016/j.ejmech.2014.06.017. Epub 2014 Jun 10.

PMID:
24946214
12.

Development of novel selective peptidomimetics containing a boronic acid moiety, targeting the 20S proteasome as anticancer agents.

Scarbaci K, Troiano V, Ettari R, Pinto A, Micale N, Di Giovanni C, Cerchia C, Schirmeister T, Novellino E, Lavecchia A, Zappalà M, Grasso S.

ChemMedChem. 2014 Aug;9(8):1801-16. doi: 10.1002/cmdc.201402075. Epub 2014 May 28.

PMID:
24891205
13.

Peptide-based proteasome inhibitors in anticancer drug design.

Micale N, Scarbaci K, Troiano V, Ettari R, Grasso S, Zappalà M.

Med Res Rev. 2014 Sep;34(5):1001-69. doi: 10.1002/med.21312. Epub 2014 Mar 1. Review.

PMID:
24585725
14.

Identification of a new series of amides as non-covalent proteasome inhibitors.

Scarbaci K, Troiano V, Micale N, Ettari R, Tamborini L, Di Giovanni C, Cerchia C, Grasso S, Novellino E, Schirmeister T, Lavecchia A, Zappalà M.

Eur J Med Chem. 2014 Apr 9;76:1-9. doi: 10.1016/j.ejmech.2014.01.022. Epub 2014 Jan 25.

PMID:
24561716
15.

Development of peptidomimetic boronates as proteasome inhibitors.

Micale N, Ettari R, Lavecchia A, Di Giovanni C, Scarbaci K, Troiano V, Grasso S, Novellino E, Schirmeister T, Zappalà M.

Eur J Med Chem. 2013 Jun;64:23-34. doi: 10.1016/j.ejmech.2013.03.032. Epub 2013 Mar 27.

PMID:
23639651
16.

Inhibition of rhodesain as a novel therapeutic modality for human African trypanosomiasis.

Ettari R, Tamborini L, Angelo IC, Micale N, Pinto A, De Micheli C, Conti P.

J Med Chem. 2013 Jul 25;56(14):5637-58. doi: 10.1021/jm301424d. Epub 2013 May 7.

PMID:
23611656
17.

Mechanism of falcipain-2 inhibition by α,β-unsaturated benzo[1,4]diazepin-2-one methyl ester.

Grazioso G, Legnani L, Toma L, Ettari R, Micale N, De Micheli C.

J Comput Aided Mol Des. 2012 Sep;26(9):1035-43. doi: 10.1007/s10822-012-9596-4. Epub 2012 Sep 11.

PMID:
22965332
18.

Synthesis and molecular modeling studies of derivatives of a highly potent peptidomimetic vinyl ester as falcipain-2 inhibitors.

Ettari R, Micale N, Grazioso G, Bova F, Schirmeister T, Grasso S, Zappalà M.

ChemMedChem. 2012 Sep;7(9):1594-600. doi: 10.1002/cmdc.201200274. Epub 2012 Jun 29.

PMID:
22753258
19.
20.

Glutamate binding-site ligands of NMDA receptors.

Bonaccorso C, Micale N, Ettari R, Grasso S, Zappalà M.

Curr Med Chem. 2011;18(36):5483-506. Review.

PMID:
22172060
21.

Selected gold compounds cause pronounced inhibition of Falcipain 2 and effectively block P. falciparum growth in vitro.

Micale N, Cinellu MA, Maiore L, Sannella AR, Severini C, Schirmeister T, Gabbiani C, Messori L.

J Inorg Biochem. 2011 Dec;105(12):1576-9. doi: 10.1016/j.jinorgbio.2011.09.006. Epub 2011 Sep 10.

PMID:
22071081
23.

Development of novel peptidomimetics containing a vinyl sulfone moiety as proteasome inhibitors.

Ettari R, Bonaccorso C, Micale N, Heindl C, Schirmeister T, Calabrò ML, Grasso S, Zappalà M.

ChemMedChem. 2011 Jul 4;6(7):1228-37. doi: 10.1002/cmdc.201100093. Epub 2011 Apr 19.

PMID:
21506279
24.

Peptidomimetics containing a vinyl ketone warhead as falcipain-2 inhibitors.

Ettari R, Zappalà M, Micale N, Grazioso G, Giofrè S, Schirmeister T, Grasso S.

Eur J Med Chem. 2011 Jun;46(6):2058-65. doi: 10.1016/j.ejmech.2011.02.058. Epub 2011 Mar 3.

PMID:
21420760
25.

Constrained peptidomimetics as antiplasmodial falcipain-2 inhibitors.

Bova F, Ettari R, Micale N, Carnovale C, Schirmeister T, Gelhaus C, Leippe M, Grasso S, Zappalà M.

Bioorg Med Chem. 2010 Jul 15;18(14):4928-38. doi: 10.1016/j.bmc.2010.06.010. Epub 2010 Jun 10.

PMID:
20598553
26.

Synthesis of novel peptidomimetics as inhibitors of protozoan cysteine proteases falcipain-2 and rhodesain.

Ettari R, Zappalà M, Micale N, Schirmeister T, Gelhaus C, Leippe M, Evers A, Grasso S.

Eur J Med Chem. 2010 Jul;45(7):3228-33. doi: 10.1016/j.ejmech.2010.04.003. Epub 2010 Apr 14.

PMID:
20434817
27.

Novel 2H-isoquinolin-3-ones as antiplasmodial falcipain-2 inhibitors.

Micale N, Ettari R, Schirmeister T, Evers A, Gelhaus C, Leippe M, Zappalà M, Grasso S.

Bioorg Med Chem. 2009 Sep 15;17(18):6505-11. doi: 10.1016/j.bmc.2009.08.013. Epub 2009 Aug 12.

PMID:
19709887
28.

Falcipain-2 inhibitors.

Ettari R, Bova F, Zappalà M, Grasso S, Micale N.

Med Res Rev. 2010 Jan;30(1):136-67. doi: 10.1002/med.20163. Review.

PMID:
19526594
29.

Novel peptidomimetics containing a vinyl ester moiety as highly potent and selective falcipain-2 inhibitors.

Ettari R, Micale N, Schirmeister T, Gelhaus C, Leippe M, Nizi E, Di Francesco ME, Grasso S, Zappalà M.

J Med Chem. 2009 Apr 9;52(7):2157-60. doi: 10.1021/jm900047j.

PMID:
19296600
30.

Synthesis, chiral resolution and pharmacological evaluation of a 2,3-benzodiazepine-derived noncompetitive AMPA receptor antagonist.

Calabrò ML, Raneri D, Ficarra P, Mennini T, Colleoni S, Grazioso G, Micale N, Zappalà M, Grasso S.

ChemMedChem. 2009 Mar;4(3):415-20. doi: 10.1002/cmdc.200800341.

PMID:
19137515
31.

N-Hydroxypyrazolyl glycine derivatives as selective N-methyl-D-aspartic acid receptor ligands.

Clausen RP, Christensen C, Hansen KB, Greenwood JR, Jørgensen L, Micale N, Madsen JC, Nielsen B, Egebjerg J, Bräuner-Osborne H, Traynelis SF, Kristensen JL.

J Med Chem. 2008 Jul 24;51(14):4179-87. doi: 10.1021/jm800025e. Epub 2008 Jun 25.

32.

Nonpeptidic vinyl and allyl phosphonates as falcipain-2 inhibitors.

Ettari R, Nizi E, Di Francesco ME, Micale N, Grasso S, Zappalà M, Vicík R, Schirmeister T.

ChemMedChem. 2008 Jul;3(7):1030-3. doi: 10.1002/cmdc.200800050. No abstract available.

PMID:
18428116
33.

Development of peptidomimetics with a vinyl sulfone warhead as irreversible falcipain-2 inhibitors.

Ettari R, Nizi E, Di Francesco ME, Dude MA, Pradel G, Vicík R, Schirmeister T, Micale N, Grasso S, Zappalà M.

J Med Chem. 2008 Feb 28;51(4):988-96. doi: 10.1021/jm701141u. Epub 2008 Jan 31.

PMID:
18232656
34.

Mechanism of inhibition of the GluR2 AMPA receptor channel opening by 2,3-benzodiazepine derivatives.

Ritz M, Micale N, Grasso S, Niu L.

Biochemistry. 2008 Jan 22;47(3):1061-9. Epub 2007 Dec 28.

PMID:
18161947
35.

Structure-activity study of 2,3-benzodiazepin-4-ones noncompetitive AMPAR antagonists: identification of the 1-(4-amino-3-methylphenyl)-3,5-dihydro-7,8-ethylenedioxy-4H-2,3-benzodiazepin-4-one as neuroprotective agent.

Micale N, Colleoni S, Postorino G, Pellicanò A, Zappalà M, Lazzaro J, Diana V, Cagnotto A, Mennini T, Grasso S.

Bioorg Med Chem. 2008 Mar 1;16(5):2200-11. Epub 2007 Dec 5.

PMID:
18083036
36.

Subunit-specific agonist activity at NR2A-, NR2B-, NR2C-, and NR2D-containing N-methyl-D-aspartate glutamate receptors.

Erreger K, Geballe MT, Kristensen A, Chen PE, Hansen KB, Lee CJ, Yuan H, Le P, Lyuboslavsky PN, Micale N, Jørgensen L, Clausen RP, Wyllie DJ, Snyder JP, Traynelis SF.

Mol Pharmacol. 2007 Oct;72(4):907-20. Epub 2007 Jul 10.

PMID:
17622578
37.

Synthesis of novel 3-(alkylcarbamoyl)-2-aryl-1,2-dihydro-6,7-(methylenedioxy)-3H-quinazolin-4-ones as anticonvulsant agents.

Micale N, Postorino G, Grasso S, Zappalà M, Zuccalà G, Ferreri G, De Sarro G.

Chem Biodivers. 2006 Mar;3(3):304-11.

PMID:
17193267
38.

Enantioseparation, absolute configuration determination, and anticonvulsant activity of (+/-)-1-(4-aminophenyl)-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-2,3-benzodiazepin-4-one.

Calabrò ML, Raneri D, Ficarra P, Ferreri G, De Sarro G, Bruno G, Zappalà M, Micale N, Grasso S.

Chirality. 2007 Jan;19(1):16-21.

PMID:
17089335
39.

Enantioselective recognition of 2,3-benzodiazepin-4-one derivatives with anticonvulsant activity on several polysaccharide chiral stationary phases.

Calabrò ML, Raneri D, Tommasini S, Ficarra R, Alcaro S, Gallelli A, Micale N, Zappalà M, Ficarra P.

J Chromatogr B Analyt Technol Biomed Life Sci. 2006 Jun 21;838(1):56-62. Epub 2006 May 24.

PMID:
16723286
40.

Novel peptidomimetic cysteine protease inhibitors as potential antimalarial agents.

Micale N, Kozikowski AP, Ettari R, Grasso S, Zappalà M, Jeong JJ, Kumar A, Hanspal M, Chishti AH.

J Med Chem. 2006 Jun 1;49(11):3064-7.

PMID:
16722625
41.

Synthesis, chiral resolution, and enantiopharmacology of a potent 2,3-benzodiazepine derivative as noncompetitive AMPA receptor antagonist.

Zappalà M, Postorino G, Micale N, Caccamese S, Parrinello N, Grazioso G, Roda G, Menniti FS, De Sarro G, Grasso S.

J Med Chem. 2006 Jan 26;49(2):575-81.

PMID:
16420043
42.

New 7,8-ethylenedioxy-2,3-benzodiazepines as noncompetitive AMPA receptor antagonists.

Zappalà M, Pellicanò A, Micale N, Menniti FS, Ferreri G, De Sarro G, Grasso S, De Micheli C.

Bioorg Med Chem Lett. 2006 Jan 1;16(1):167-70. Epub 2005 Oct 10.

PMID:
16216501
43.

Synthesis of 2-semicarbazonomethyl-4,5-methylenedioxyphenylacetic acids as anticonvulsant agents.

Micale N, Zappalà M, Zuccalà G, Menniti FS, Ferreri G, De Sarro G, Grasso S.

Farmaco. 2005 Mar;60(3):231-5.

PMID:
15784242
44.

Design and synthesis of a potent and selective peptidomimetic inhibitor of caspase-3.

Micale N, Vairagoundar R, Yakovlev AG, Kozikowski AP.

J Med Chem. 2004 Dec 16;47(26):6455-8.

PMID:
15588079
45.

Design of 1-substituted 2-arylmethyl-4,5-methylenedioxybenzene derivatives as antiseizure agents.

Micale N, De Sarro G, Ferreri G, Zappalá M, Grasso S, Puia G, De Micheli C.

Bioorg Med Chem. 2004 Jul 1;12(13):3703-9.

PMID:
15186856
46.

1-aryl-6,7-methylenedioxy-3H-quinazolin-4-ones as anticonvulsant agents.

Zappalà M, Grasso S, Micale N, Zuccalà G, Menniti FS, Ferreri G, De Sarro G, De Micheli C.

Bioorg Med Chem Lett. 2003 Dec 15;13(24):4427-30.

PMID:
14643339
47.

Synthesis and cytotoxic activity of 1,3-benzodioxole derivatives. Note II.

Micale N, Zappalà M, Grasso S.

Farmaco. 2003 May;58(5):351-5.

PMID:
12729828
48.

5-phenyl-9H-1,3-dioxolo[4,5-h][2,3]benzodiazepin-8(7H)-one.

Bruno G, Nicoló F, Gitto R, Micale N, Rosace G.

Acta Crystallogr C. 2003 Mar;59(Pt 3):o117-9. Epub 2003 Feb 11.

PMID:
12711781
49.

Characterization of the mechanism of anticonvulsant activity for a selected set of putative AMPA receptor antagonists.

Grasso S, Micale N, Zappalà M, Galli A, Costagli C, Menniti FS, De Micheli C.

Bioorg Med Chem Lett. 2003 Feb 10;13(3):443-6.

PMID:
12565947
50.

Synthesis and antitumor activity of 1,3-benzodioxole derivatives.

Micale N, Zappalà M, Grasso S.

Farmaco. 2002 Oct;57(10):853-9.

PMID:
12420881

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