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Items: 1 to 20 of 52

1.

Pyrazole and imidazo[1,2-b]pyrazole Derivatives as New Potential Antituberculosis Agents.

Meta E, Brullo C, Tonelli M, Franzblau SG, Wang Y, Ma R, Baojie W, Orena BS, Pasca MR, Bruno O.

Med Chem. 2019;15(1):17-27. doi: 10.2174/1573406414666180524084023.

PMID:
29792151
2.

Molecular Bases of PDE4D Inhibition by Memory-Enhancing GEBR Library Compounds.

Prosdocimi T, Mollica L, Donini S, Semrau MS, Lucarelli AP, Aiolfi E, Cavalli A, Storici P, Alfei S, Brullo C, Bruno O, Parisini E.

Biochemistry. 2018 May 15;57(19):2876-2888. doi: 10.1021/acs.biochem.8b00288. Epub 2018 May 1.

PMID:
29652483
3.

The pyrazolyl-urea GeGe3 inhibits tumor angiogenesis and reveals dystrophia myotonica protein kinase (DMPK)1 as a novel angiogenesis target.

Meta E, Imhof BA, Ropraz P, Fish RJ, Brullo C, Bruno O, Sidibé A.

Oncotarget. 2017 Nov 21;8(64):108195-108212. doi: 10.18632/oncotarget.22598. eCollection 2017 Dec 8.

4.

Memory-enhancing effects of GEBR-32a, a new PDE4D inhibitor holding promise for the treatment of Alzheimer's disease.

Ricciarelli R, Brullo C, Prickaerts J, Arancio O, Villa C, Rebosio C, Calcagno E, Balbi M, van Hagen BT, Argyrousi EK, Zhang H, Pronzato MA, Bruno O, Fedele E.

Sci Rep. 2017 Apr 12;7:46320. doi: 10.1038/srep46320.

5.

Design, synthesis and biological evaluation of new pyrazolyl-ureas and imidazopyrazolecarboxamides able to interfere with MAPK and PI3K upstream signaling involved in the angiogenesis.

Meta E, Brullo C, Sidibe A, Imhof BA, Bruno O.

Eur J Med Chem. 2017 Jun 16;133:24-35. doi: 10.1016/j.ejmech.2017.03.066. Epub 2017 Mar 27.

PMID:
28371678
6.

Benzimidazole-based derivatives as privileged scaffold developed for the treatment of the RSV infection: a computational study exploring the potency and cytotoxicity profiles.

Cichero E, Tonelli M, Novelli F, Tasso B, Delogu I, Loddo R, Bruno O, Fossa P.

J Enzyme Inhib Med Chem. 2017 Dec;32(1):375-402. doi: 10.1080/14756366.2016.1256881.

7.

Design and synthesis of 4,5,6,7-tetrahydro-1H-1,2-diazepin-7-one derivatives as a new series of Phosphodiesterase 4 (PDE4) inhibitors.

Guariento S, Karawajczyk A, Bull JA, Marchini G, Bielska M, Iwanowa X, Bruno O, Fossa P, Giordanetto F.

Bioorg Med Chem Lett. 2017 Jan 1;27(1):24-29. doi: 10.1016/j.bmcl.2016.11.040. Epub 2016 Nov 16.

PMID:
27890378
8.

New insights into selective PDE4D inhibitors: 3-(Cyclopentyloxy)-4-methoxybenzaldehyde O-(2-(2,6-dimethylmorpholino)-2-oxoethyl) oxime (GEBR-7b) structural development and promising activities to restore memory impairment.

Brullo C, Ricciarelli R, Prickaerts J, Arancio O, Massa M, Rotolo C, Romussi A, Rebosio C, Marengo B, Pronzato MA, van Hagen BTJ, van Goethem NP, D'Ursi P, Orro A, Milanesi L, Guariento S, Cichero E, Fossa P, Fedele E, Bruno O.

Eur J Med Chem. 2016 Nov 29;124:82-102. doi: 10.1016/j.ejmech.2016.08.018. Epub 2016 Aug 13.

PMID:
27560284
9.

Further Insights in the Binding Mode of Selective Inhibitors to Human PDE4D Enzyme Combining Docking and Molecular Dynamics.

D'Ursi P, Guariento S, Trombetti G, Orro A, Cichero E, Milanesi L, Fossa P, Bruno O.

Mol Inform. 2016 Sep;35(8-9):369-81. doi: 10.1002/minf.201501033. Epub 2016 Jun 20.

10.

New insights into PDE4B inhibitor selectivity: CoMFA analyses and molecular docking studies.

Guariento S, Bruno O, Fossa P, Cichero E.

Mol Divers. 2016 Feb;20(1):77-92. doi: 10.1007/s11030-015-9631-1. Epub 2015 Aug 20.

PMID:
26290462
11.

Synthesis, biological activities and pharmacokinetic properties of new fluorinated derivatives of selective PDE4D inhibitors.

Brullo C, Massa M, Villa C, Ricciarelli R, Rivera D, Pronzato MA, Fedele E, Barocelli E, Bertoni S, Flammini L, Bruno O.

Bioorg Med Chem. 2015 Jul 1;23(13):3426-35. doi: 10.1016/j.bmc.2015.04.027. Epub 2015 Apr 16.

PMID:
25936260
12.

Synthesis, biological evaluation, and molecular modeling of new 3-(cyclopentyloxy)-4-methoxybenzaldehyde O-(2-(2,6-dimethylmorpholino)-2-oxoethyl) Oxime (GEBR-7b) related phosphodiesterase 4D (PDE4D) inhibitors.

Brullo C, Massa M, Rocca M, Rotolo C, Guariento S, Rivera D, Ricciarelli R, Fedele E, Fossa P, Bruno O.

J Med Chem. 2014 Aug 28;57(16):7061-72. doi: 10.1021/jm500855w. Epub 2014 Aug 15.

PMID:
25126889
13.

PDE4D inhibitors: a potential strategy for the treatment of memory impairment?

Bruno O, Ricciarelli R, Prickaerts J, Parker L, Fedele E.

Neuropharmacology. 2014 Oct;85:290-2. doi: 10.1016/j.neuropharm.2014.05.038. Epub 2014 Jun 2. No abstract available.

PMID:
24942130
14.

A novel mechanism for cyclic adenosine monophosphate-mediated memory formation: Role of amyloid beta.

Ricciarelli R, Puzzo D, Bruno O, Canepa E, Gardella E, Rivera D, Privitera L, Domenicotti C, Marengo B, Marinari UM, Palmeri A, Pronzato MA, Arancio O, Fedele E.

Ann Neurol. 2014 Apr;75(4):602-7. doi: 10.1002/ana.24130. Epub 2014 Apr 14.

PMID:
24591104
15.

Differential inhibition of signaling pathways by two new imidazo-pyrazoles molecules in fMLF-OMe- and IL8-stimulated human neutrophil.

Selvatici R, Brullo C, Bruno O, Spisani S.

Eur J Pharmacol. 2013 Oct 15;718(1-3):428-34. doi: 10.1016/j.ejphar.2013.07.045. Epub 2013 Aug 23.

PMID:
23978569
16.

Homology modeling, docking studies and molecular dynamic simulations using graphical processing unit architecture to probe the type-11 phosphodiesterase catalytic site: a computational approach for the rational design of selective inhibitors.

Cichero E, D'Ursi P, Moscatelli M, Bruno O, Orro A, Rotolo C, Milanesi L, Fossa P.

Chem Biol Drug Des. 2013 Dec;82(6):718-31. doi: 10.1111/cbdd.12193. Epub 2013 Aug 26.

PMID:
23865680
17.

Phosphodiesterase isoform-specific expression induced by traumatic brain injury.

Oliva AA Jr, Kang Y, Furones C, Alonso OF, Bruno O, Dietrich WD, Atkins CM.

J Neurochem. 2012 Dec;123(6):1019-29. doi: 10.1111/jnc.12049. Epub 2012 Nov 1.

18.

Synthesis of new 5,6-dihydrobenzo[h]quinazoline 2,4-diamino substituted and antiplatelet/antiphlogistic activities evaluation.

Brullo C, Rocca M, Fossa P, Cichero E, Barocelli E, Ballabeni V, Flammini L, Giorgio C, Saccani F, Domenichini G, Bruno O.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1125-9. doi: 10.1016/j.bmcl.2011.11.103. Epub 2011 Dec 3.

PMID:
22189137
19.

N-Aryl-2-phenyl-2,3-dihydro-imidazo[1,2-b]pyrazole-1-carboxamides 7-substituted strongly inhibiting both fMLP-OMe- and IL-8-induced human neutrophil chemotaxis.

Brullo C, Spisani S, Selvatici R, Bruno O.

Eur J Med Chem. 2012 Jan;47(1):573-9. doi: 10.1016/j.ejmech.2011.11.031. Epub 2011 Nov 25.

PMID:
22152986
20.

Docking-based CoMFA and CoMSIA analyses of tetrahydro-β-carboline derivatives as type-5 phosphodiesterase inhibitors.

Cichero E, Bruno O, Fossa P.

J Enzyme Inhib Med Chem. 2012 Oct;27(5):730-43. doi: 10.3109/14756366.2011.611136. Epub 2011 Oct 21.

PMID:
22014072

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