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Items: 1 to 50 of 138

1.

A thiazepino[4,5-a]benzimidazole derivative hampers the RNA replication of Eurasian serotypes of foot-and-mouth disease virus.

Lefebvre DJ, De Vleeschauwer AR, Goris N, Van Borm S, Chimirri A, Monforte AM, Valdazo-Gonzalez B, King DP, Neyts J, De Clercq K.

Biochem Biophys Res Commun. 2014 Dec 12;455(3-4):378-81. doi: 10.1016/j.bbrc.2014.11.023. Epub 2014 Nov 15.

PMID:
25446115
2.

Diketoacid chelating ligands as dual inhibitors of HIV-1 integration process.

Rogolino D, Carcelli M, Compari C, De Luca L, Ferro S, Fisicaro E, Rispoli G, Neamati N, Debyser Z, Christ F, Chimirri A.

Eur J Med Chem. 2014 May 6;78:425-30. doi: 10.1016/j.ejmech.2014.03.070. Epub 2014 Mar 25.

PMID:
24704615
3.

A new potential approach to block HIV-1 replication via protein-protein interaction and strand-transfer inhibition.

Ferro S, De Luca L, Lo Surdo G, Morreale F, Christ F, Debyser Z, Gitto R, Chimirri A.

Bioorg Med Chem. 2014 Apr 1;22(7):2269-79. doi: 10.1016/j.bmc.2014.02.012. Epub 2014 Feb 20.

PMID:
24618511
4.

Design and synthesis of N₁-aryl-benzimidazoles 2-substituted as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.

Monforte AM, Ferro S, De Luca L, Lo Surdo G, Morreale F, Pannecouque C, Balzarini J, Chimirri A.

Bioorg Med Chem. 2014 Feb 15;22(4):1459-67. doi: 10.1016/j.bmc.2013.12.045. Epub 2013 Dec 30.

PMID:
24457088
5.

Synthesis, modelling and biological characterization of 3-substituted-1H-indoles as ligands of GluN2B-containing N-methyl-d-aspartate receptors.

Gitto R, De Luca L, Ferro S, Russo E, De Sarro G, Chisari M, Ciranna L, Alvarez-Builla J, Alajarin R, Buemi MR, Chimirri A.

Bioorg Med Chem. 2014 Feb 1;22(3):1040-8. doi: 10.1016/j.bmc.2013.12.040. Epub 2013 Dec 30.

PMID:
24411196
6.

From NMDA receptor antagonists to discovery of selective σ₂ receptor ligands.

Gitto R, De Luca L, Ferro S, Scala A, Ronsisvalle S, Parenti C, Prezzavento O, Buemi MR, Chimirri A.

Bioorg Med Chem. 2014 Jan 1;22(1):393-7. doi: 10.1016/j.bmc.2013.11.014. Epub 2013 Nov 15.

PMID:
24290063
7.

Structure-based screening for the discovery of new carbonic anhydrase VII inhibitors.

De Luca L, Ferro S, Damiano FM, Supuran CT, Vullo D, Chimirri A, Gitto R.

Eur J Med Chem. 2014 Jan;71:105-11. doi: 10.1016/j.ejmech.2013.10.071. Epub 2013 Nov 8.

PMID:
24287559
8.

Synthesis and biological evaluation of novel antiviral agents as protein-protein interaction inhibitors.

Ferro S, De Luca L, Morreale F, Christ F, Debyser Z, Gitto R, Chimirri A.

J Enzyme Inhib Med Chem. 2014 Apr;29(2):237-42. doi: 10.3109/14756366.2013.766609. Epub 2013 Jul 16.

PMID:
23859152
9.

Indole derivatives as dual-effective agents for the treatment of neurodegenerative diseases: synthesis, biological evaluation, and molecular modeling studies.

Buemi MR, De Luca L, Chimirri A, Ferro S, Gitto R, Alvarez-Builla J, Alajarin R.

Bioorg Med Chem. 2013 Aug 1;21(15):4575-80. doi: 10.1016/j.bmc.2013.05.044. Epub 2013 Jun 2.

PMID:
23777828
10.

Insight into the fundamental interactions between LEDGF binding site inhibitors and integrase combining docking and molecular dynamics simulations.

De Luca L, Morreale F, Chimirri A.

J Chem Inf Model. 2012 Dec 21;52(12):3245-54. doi: 10.1021/ci300361e. Epub 2012 Dec 11.

PMID:
23194297
11.

Synthesis and biological characterization of 3-substituted 1H-indoles as ligands of GluN2B-containing N-methyl-D-aspartate receptors. Part 2.

Gitto R, De Luca L, Ferro S, Buemi MR, Russo E, De Sarro G, Chisari M, Ciranna L, Chimirri A.

J Med Chem. 2012 Dec 13;55(23):10532-9. doi: 10.1021/jm301508d. Epub 2012 Nov 19.

PMID:
23140383
12.

Fragment hopping approach directed at design of HIV IN-LEDGF/p75 interaction inhibitors.

De Luca L, Ferro S, Morreale F, Christ F, Debyser Z, Chimirri A, Gitto R.

J Enzyme Inhib Med Chem. 2013 Oct;28(5):1002-9. doi: 10.3109/14756366.2012.703184. Epub 2012 Jul 18.

PMID:
22803661
13.

New AMPA antagonists in epilepsy.

Russo E, Gitto R, Citraro R, Chimirri A, De Sarro G.

Expert Opin Investig Drugs. 2012 Sep;21(9):1371-89. doi: 10.1517/13543784.2012.705277. Epub 2012 Jul 13. Review.

PMID:
22788917
14.

Synthesis, structure-activity relationship studies, and X-ray crystallographic analysis of arylsulfonamides as potent carbonic anhydrase inhibitors.

Gitto R, Damiano FM, Mader P, De Luca L, Ferro S, Supuran CT, Vullo D, Brynda J, Rezáčová P, Chimirri A.

J Med Chem. 2012 Apr 26;55(8):3891-9. doi: 10.1021/jm300112w. Epub 2012 Apr 6.

PMID:
22443141
15.

Glutamatergic neurotransmission as molecular target of new anticonvulsants.

Gitto R, De Luca L, De Grazia S, Chimirri A.

Curr Top Med Chem. 2012;12(9):971-93. Review.

PMID:
22352860
16.

Synthesis and biological characterization of 3-substituted-1H-indoles as ligands of GluN2B-containing N-methyl-D-aspartate receptors.

Gitto R, De Luca L, Ferro S, Buemi MR, Russo E, De Sarro G, Costa L, Ciranna L, Prezzavento O, Arena E, Ronsisvalle S, Bruno G, Chimirri A.

J Med Chem. 2011 Dec 22;54(24):8702-6. doi: 10.1021/jm2008002. Epub 2011 Nov 16.

PMID:
22050212
17.

Synthesis and biological profile of new 1,2,3,4-tetrahydroisoquinolines as selective carbonic anhydrase inhibitors.

Gitto R, Damiano FM, De Luca L, Ferro S, Vullo D, Supuran CT, Chimirri A.

Bioorg Med Chem. 2011 Dec 1;19(23):7003-7. doi: 10.1016/j.bmc.2011.10.015. Epub 2011 Oct 12.

PMID:
22041171
18.

Microwave assisted organic synthesis (MAOS) of small molecules as potential HIV-1 integrase inhibitors.

Ferro S, Grazia SD, De Luca L, Gitto R, Faliti CE, Debyzer Z, Chimirri A.

Molecules. 2011 Aug 11;16(8):6858-70. doi: 10.3390/molecules16086858.

19.

4-[1-(4-Fluorobenzyl)-4-hydroxy-1H-indol-3-yl]-2-hydroxy-4-oxobut-2-enoic acid as a prototype to develop dual inhibitors of HIV-1 integration process.

De Luca L, Gitto R, Christ F, Ferro S, De Grazia S, Morreale F, Debyser Z, Chimirri A.

Antiviral Res. 2011 Oct;92(1):102-7. doi: 10.1016/j.antiviral.2011.07.005. Epub 2011 Jul 13.

PMID:
21767569
20.

3-[2-(1H-1,3-Benzodiazol-2-yl)eth-yl]-1,3-oxazolidin-2-one.

Brancatelli G, Nicoló F, De Grazia S, Monforte AM, Chimirri A.

Acta Crystallogr Sect E Struct Rep Online. 2011 May 1;67(Pt 5):o1083. doi: 10.1107/S1600536811012256. Epub 2011 Apr 13.

21.

Inhibition of the interaction between HIV-1 integrase and its cofactor LEDGF/p75: a promising approach in anti-retroviral therapy.

De Luca L, Ferro S, Morreale F, Chimirri A.

Mini Rev Med Chem. 2011 Jul;11(8):714-27. Review.

PMID:
21651465
22.

Inhibitors of the interactions between HIV-1 IN and the cofactor LEDGF/p75.

De Luca L, Ferro S, Morreale F, De Grazia S, Chimirri A.

ChemMedChem. 2011 Jul 4;6(7):1184-91. doi: 10.1002/cmdc.201100071. Epub 2011 Apr 19. Review.

PMID:
21506277
23.

Structural basis for the interaction between carbonic anhydrase and 1,2,3,4-tetrahydroisoquinolin-2-ylsulfonamides.

Mader P, Brynda J, Gitto R, Agnello S, Pachl P, Supuran CT, Chimirri A, Řezáčová P.

J Med Chem. 2011 Apr 14;54(7):2522-6. doi: 10.1021/jm2000213. Epub 2011 Mar 11.

PMID:
21395315
24.

HIV-1 integrase strand-transfer inhibitors: design, synthesis and molecular modeling investigation.

De Luca L, De Grazia S, Ferro S, Gitto R, Christ F, Debyser Z, Chimirri A.

Eur J Med Chem. 2011 Feb;46(2):756-64. doi: 10.1016/j.ejmech.2010.12.012. Epub 2010 Dec 21.

PMID:
21227550
25.

2-hydroxyisoquinoline-1,3(2H,4H)-diones as inhibitors of HIV-1 integrase and reverse transcriptase RNase H domain: influence of the alkylation of position 4.

Billamboz M, Bailly F, Lion C, Calmels C, Andréola ML, Witvrouw M, Christ F, Debyser Z, De Luca L, Chimirri A, Cotelle P.

Eur J Med Chem. 2011 Feb;46(2):535-46. doi: 10.1016/j.ejmech.2010.11.033. Epub 2010 Nov 27.

PMID:
21185110
26.

Synthesis and structure-active relationship of 1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline anticonvulsants.

Gitto R, De Luca L, Ferro S, Agnello S, Russo E, De Sarro G, Chimirri A.

Chem Pharm Bull (Tokyo). 2010 Dec;58(12):1602-5.

27.

Small molecules targeting the interaction between HIV-1 integrase and LEDGF/p75 cofactor.

De Luca L, Ferro S, Gitto R, Barreca ML, Agnello S, Christ F, Debyser Z, Chimirri A.

Bioorg Med Chem. 2010 Nov 1;18(21):7515-21. doi: 10.1016/j.bmc.2010.08.051. Epub 2010 Sep 17.

PMID:
20850978
28.

New chloro,fluorobenzylindole derivatives as integrase strand-transfer inhibitors (INSTIs) and their mode of action.

Ferro S, De Luca L, Barreca ML, De Grazia S, Christ F, Debyser Z, Chimirri A.

Bioorg Med Chem. 2010 Aug 1;18(15):5510-8. doi: 10.1016/j.bmc.2010.06.063. Epub 2010 Jun 22.

PMID:
20630765
29.

Identification of potent and selective human carbonic anhydrase VII (hCA VII) inhibitors.

Gitto R, Agnello S, Ferro S, Vullo D, Supuran CT, Chimirri A.

ChemMedChem. 2010 Jun 7;5(6):823-6. doi: 10.1002/cmdc.201000044. No abstract available.

PMID:
20349499
30.

Slow binding-tight binding interaction between benzimidazol-2-one inhibitors and HIV-1 reverse transcriptase containing the lysine 103 to asparagine mutation.

Samuele A, Crespan E, Vitellaro S, Monforte AM, Logoteta P, Chimirri A, Maga G.

Antiviral Res. 2010 Jun;86(3):268-75. doi: 10.1016/j.antiviral.2010.03.008. Epub 2010 Mar 20.

PMID:
20307579
31.

Identification of 3,4-Dihydroisoquinoline-2(1H)-sulfonamides as potent carbonic anhydrase inhibitors: synthesis, biological evaluation, and enzyme--ligand X-ray studies.

Gitto R, Agnello S, Ferro S, De Luca L, Vullo D, Brynda J, Mader P, Supuran CT, Chimirri A.

J Med Chem. 2010 Mar 25;53(6):2401-8. doi: 10.1021/jm9014026.

PMID:
20170095
32.

Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.

Monforte AM, Logoteta P, De Luca L, Iraci N, Ferro S, Maga G, De Clercq E, Pannecouque C, Chimirri A.

Bioorg Med Chem. 2010 Feb 15;18(4):1702-10. doi: 10.1016/j.bmc.2009.12.059. Epub 2010 Jan 4.

PMID:
20097079
33.

Design, synthesis, and structure-activity relationships of 1,3-dihydrobenzimidazol-2-one analogues as anti-HIV agents.

Monforte AM, Logoteta P, Ferro S, De Luca L, Iraci N, Maga G, Clercq ED, Pannecouque C, Chimirri A.

Bioorg Med Chem. 2009 Aug 15;17(16):5962-7. doi: 10.1016/j.bmc.2009.06.068. Epub 2009 Jul 3.

PMID:
19616956
34.

Pharmacophore-based discovery of small-molecule inhibitors of protein-protein interactions between HIV-1 integrase and cellular cofactor LEDGF/p75.

De Luca L, Barreca ML, Ferro S, Christ F, Iraci N, Gitto R, Monforte AM, Debyser Z, Chimirri A.

ChemMedChem. 2009 Aug;4(8):1311-6. doi: 10.1002/cmdc.200900070.

PMID:
19565598
35.

Induced-fit docking approach provides insight into the binding mode and mechanism of action of HIV-1 integrase inhibitors.

Barreca ML, Iraci N, De Luca L, Chimirri A.

ChemMedChem. 2009 Sep;4(9):1446-56. doi: 10.1002/cmdc.200900166.

PMID:
19544345
36.

Combined strategies for the discovery of ionotropic glutamate receptor antagonists.

Chimirri A, De Luca L, Ferro S, De Sarro G, Ciranna L, Gitto R.

ChemMedChem. 2009 Jun;4(6):917-22. doi: 10.1002/cmdc.200900109. Review.

PMID:
19422004
37.

Synthesis and evaluation of pharmacological profile of 1-aryl-6,7-dimethoxy-3,4-dihydroisoquinoline-2(1H)-sulfonamides.

Gitto R, Ferro S, Agnello S, De Luca L, De Sarro G, Russo E, Vullo D, Supuran CT, Chimirri A.

Bioorg Med Chem. 2009 May 15;17(10):3659-64. doi: 10.1016/j.bmc.2009.03.066. Epub 2009 Apr 7.

PMID:
19398204
38.

Development of 3-substituted-1H-indole derivatives as NR2B/NMDA receptor antagonists.

Gitto R, De Luca L, Ferro S, Citraro R, De Sarro G, Costa L, Ciranna L, Chimirri A.

Bioorg Med Chem. 2009 Feb 15;17(4):1640-7. doi: 10.1016/j.bmc.2008.12.058. Epub 2008 Dec 31.

PMID:
19157884
39.

Docking studies on a new human immunodeficiency virus integrase-Mg-DNA complex: phenyl ring exploration and synthesis of 1H-benzylindole derivatives through fluorine substitutions.

Ferro S, De Luca L, Barreca ML, Iraci N, De Grazia S, Christ F, Witvrouw M, Debyser Z, Chimirri A.

J Med Chem. 2009 Jan 22;52(2):569-73. doi: 10.1021/jm8009266.

PMID:
19105658
40.

Computational studies to discover a new NR2B/NMDA receptor antagonist and evaluation of pharmacological profile.

Gitto R, De Luca L, Ferro S, Occhiuto F, Samperi S, De Sarro G, Russo E, Ciranna L, Costa L, Chimirri A.

ChemMedChem. 2008 Oct;3(10):1539-48. doi: 10.1002/cmdc.200800124.

PMID:
18767069
41.

Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors.

Monforte AM, Rao A, Logoteta P, Ferro S, De Luca L, Barreca ML, Iraci N, Maga G, De Clercq E, Pannecouque C, Chimirri A.

Bioorg Med Chem. 2008 Aug 1;16(15):7429-35. doi: 10.1016/j.bmc.2008.06.012. Epub 2008 Jun 13.

PMID:
18585918
42.

Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.

Hombrouck A, Van Remoortel B, Michiels M, Noppe W, Christ F, Eneroth A, Sahlberg BL, Benkestock K, Vrang L, Johansson NG, Barreca ML, De Luca L, Ferro S, Chimirri A, Debyser Z, Witvrouw M.

Antimicrob Agents Chemother. 2008 Aug;52(8):2861-9. doi: 10.1128/AAC.00210-08. Epub 2008 Jun 9.

43.

Enhancement of anti-absence effects of ethosuximide by low doses of a noncompetitive alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonist in a genetic animal model of absence epilepsy.

Russo E, Citraro R, De Fazio S, Marra R, Gitto R, Chimirri A, De Sarro G, Di Paola ED.

Epilepsy Behav. 2008 Aug;13(2):295-9. doi: 10.1016/j.yebeh.2008.04.018. Epub 2008 Jun 2.

PMID:
18514580
44.

A refined pharmacophore model for HIV-1 integrase inhibitors: Optimization of potency in the 1H-benzylindole series.

De Luca L, Barreca ML, Ferro S, Iraci N, Michiels M, Christ F, Debyser Z, Witvrouw M, Chimirri A.

Bioorg Med Chem Lett. 2008 May 1;18(9):2891-5. doi: 10.1016/j.bmcl.2008.03.089. Epub 2008 Apr 8.

PMID:
18417342
45.

Solution-phase parallel synthesis and evaluation of anticonvulsant activity of N-substituted-3,4-dihydroisoquinoline-2(1H)-carboxamides.

Gitto R, Pagano B, Citraro R, Scicchitano F, De Sarro G, Chimirri A.

Eur J Med Chem. 2009 Mar;44(3):1349-54. doi: 10.1016/j.ejmech.2008.02.025. Epub 2008 Mar 7.

PMID:
18406016
46.

The thiazolobenzimidazole TBZE-029 inhibits enterovirus replication by targeting a short region immediately downstream from motif C in the nonstructural protein 2C.

De Palma AM, Heggermont W, Lanke K, Coutard B, Bergmann M, Monforte AM, Canard B, De Clercq E, Chimirri A, Pürstinger G, Rohayem J, van Kuppeveld F, Neyts J.

J Virol. 2008 May;82(10):4720-30. doi: 10.1128/JVI.01338-07. Epub 2008 Mar 12.

47.

Solution-phase parallel synthesis of novel 1,2,3,4-tetrahydroisoquinoline-1-ones as anticonvulsant agents.

Gitto R, Francica E, De Sarro G, Scicchitano F, Chimirri A.

Chem Pharm Bull (Tokyo). 2008 Feb;56(2):181-4.

48.

Synthesis and anticonvulsant evaluation of N-substituted isoquinoline AMPA receptor antagonists.

Gitto R, De Luca L, Pagano B, Citraro R, De Sarro G, Costa L, Ciranna L, Chimirri A.

Bioorg Med Chem. 2008 Mar 1;16(5):2379-84. Epub 2007 Nov 29.

PMID:
18077172
49.

Human immunodeficiency virus integrase inhibitors efficiently suppress feline immunodeficiency virus replication in vitro and provide a rationale to redesign antiretroviral treatment for feline AIDS.

Savarino A, Pistello M, D'Ostilio D, Zabogli E, Taglia F, Mancini F, Ferro S, Matteucci D, De Luca L, Barreca ML, Ciervo A, Chimirri A, Ciccozzi M, Bendinelli M.

Retrovirology. 2007 Oct 30;4:79.

50.

Tn5 transposase as a useful platform to simulate HIV-1 integrase inhibitor binding mode.

Barreca ML, Ortuso F, Iraci N, De Luca L, Alcaro S, Chimirri A.

Biochem Biophys Res Commun. 2007 Nov 23;363(3):554-60. Epub 2007 Sep 14.

PMID:
17889829

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