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Items: 1 to 50 of 87

1.

Investigation of the Role of Chirality in the Interaction with σ Receptors and Effect on Binge Eating Episode of a Potent σ1 Antagonist Analogue of Spipethiane.

Del Bello F, Micioni Di Bonaventura MV, Bonifazi A, Wünsch B, Schepmann D, Giancola JB, Micioni Di Bonaventura E, Vistoli G, Giorgioni G, Quaglia W, Piergentili A, Cifani C.

ACS Chem Neurosci. 2019 Aug 21;10(8):3391-3397. doi: 10.1021/acschemneuro.9b00261. Epub 2019 Jul 23.

PMID:
31298830
2.

Role of the NMDA Receptor in the Antitumor Activity of Chiral 1,4-Dioxane Ligands in MCF-7 and SKBR3 Breast Cancer Cells.

Morelli MB, Amantini C, Nabissi M, Santoni G, Wünsch B, Schepmann D, Cimarelli C, Pellei M, Santini C, Fontana S, Mammoli V, Quaglia W, Bonifazi A, Giannella M, Giorgioni G, Piergentili A, Del Bello F.

ACS Med Chem Lett. 2019 Jan 28;10(4):511-516. doi: 10.1021/acsmedchemlett.8b00536. eCollection 2019 Apr 11.

PMID:
30996788
3.

Receptor Ligands as Helping Hands to L-DOPA in the Treatment of Parkinson's Disease.

Del Bello F, Giannella M, Giorgioni G, Piergentili A, Quaglia W.

Biomolecules. 2019 Apr 9;9(4). pii: E142. doi: 10.3390/biom9040142. Review.

4.

Chemical manipulations on the 1,4-dioxane ring of 5-HT1A receptor agonists lead to antagonists endowed with antitumor activity in prostate cancer cells.

Del Bello F, Bonifazi A, Giorgioni G, Quaglia W, Amantini C, Morelli MB, Santoni G, Battiti FO, Vistoli G, Cilia A, Piergentili A.

Eur J Med Chem. 2019 Apr 15;168:461-473. doi: 10.1016/j.ejmech.2019.02.056. Epub 2019 Feb 25.

PMID:
30844609
5.

Multitarget 1,4-Dioxane Compounds Combining Favorable D2-like and 5-HT1A Receptor Interactions with Potential for the Treatment of Parkinson's Disease or Schizophrenia.

Del Bello F, Ambrosini D, Bonifazi A, Newman AH, Keck TM, Giannella M, Giorgioni G, Piergentili A, Cappellacci L, Cilia A, Franchini S, Quaglia W.

ACS Chem Neurosci. 2019 May 15;10(5):2222-2228. doi: 10.1021/acschemneuro.8b00677. Epub 2019 Jan 9.

PMID:
30609891
6.

Syntheses and biological studies of nitroimidazole conjugated heteroscorpionate ligands and related Cu(I) and Cu(II) complexes.

Pellei M, Gandin V, Cimarelli C, Quaglia W, Mosca N, Bagnarelli L, Marzano C, Santini C.

J Inorg Biochem. 2018 Oct;187:33-40. doi: 10.1016/j.jinorgbio.2018.07.008. Epub 2018 Jul 19.

PMID:
30053534
7.

1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D4 Receptor.

Del Bello F, Bonifazi A, Giorgioni G, Cifani C, Micioni Di Bonaventura MV, Petrelli R, Piergentili A, Fontana S, Mammoli V, Yano H, Matucci R, Vistoli G, Quaglia W.

J Med Chem. 2018 Apr 26;61(8):3712-3725. doi: 10.1021/acs.jmedchem.8b00265. Epub 2018 Apr 6.

PMID:
29589445
8.

Synergic stimulation of serotonin 5-HT1A receptor and α2-adrenoceptors for neuropathic pain relief: Preclinical effects of 2-substituted imidazoline derivatives.

Di Cesare Mannelli L, Ghelardini C, Micheli L, Del Bello F, Giannella M, Piergentili A, Pigini M, Quaglia W.

Eur J Pharmacol. 2017 Sep 5;810:128-133. doi: 10.1016/j.ejphar.2017.06.023. Epub 2017 Jun 17.

PMID:
28633926
9.

Novel muscarinic acetylcholine receptor hybrid ligands embedding quinuclidine and 1,4-dioxane fragments.

Del Bello F, Bonifazi A, Giorgioni G, Petrelli R, Quaglia W, Altomare A, Falcicchio A, Matucci R, Vistoli G, Piergentili A.

Eur J Med Chem. 2017 Sep 8;137:327-337. doi: 10.1016/j.ejmech.2017.06.004. Epub 2017 Jun 3.

PMID:
28609709
10.

Nano-medicine Improving the Bioavailability of Small Molecules for the Prevention of Neurodegenerative Diseases.

Di Martino P, Censi R, Gigliobianco MR, Zerrillo L, Magnoni F, Agas D, Quaglia W, Lupidi G.

Curr Pharm Des. 2017;23(13):1897-1908. doi: 10.2174/1381612822666161227154447. Review.

PMID:
28025942
11.

Combined Interactions with I1-, I2-Imidazoline Binding Sites and α2-Adrenoceptors To Manage Opioid Addiction.

Giusepponi ME, Cifani C, Micioni Di Bonaventura MV, Mattioli L, Hudson A, Diamanti E, Del Bello F, Giannella M, Mammoli V, Paoletti CD, Piergentili A, Pigini M, Quaglia W.

ACS Med Chem Lett. 2016 Sep 8;7(10):956-961. eCollection 2016 Oct 13.

12.

The Versatile 2-Substituted Imidazoline Nucleus as a Structural Motif of Ligands Directed to the Serotonin 5-HT1A Receptor.

Del Bello F, Cilia A, Carrieri A, Fasano DC, Ghelardini C, Di Cesare Mannelli L, Micheli L, Santini C, Diamanti E, Giannella M, Giorgioni G, Mammoli V, Paoletti CD, Petrelli R, Piergentili A, Quaglia W, Pigini M.

ChemMedChem. 2016 Oct 19;11(20):2287-2298. doi: 10.1002/cmdc.201600383. Epub 2016 Sep 30.

PMID:
27690321
13.

The replacement of the 2-methoxy substituent of N-((6,6-diphenyl-1,4-dioxan-2-yl)methyl)-2-(2-methoxyphenoxy)ethan-1-amine improves the selectivity for 5-HT1A receptor over α1-adrenoceptor and D2-like receptor subtypes.

Del Bello F, Bonifazi A, Giannella M, Giorgioni G, Piergentili A, Petrelli R, Cifani C, Micioni Di Bonaventura MV, Keck TM, Mazzolari A, Vistoli G, Cilia A, Poggesi E, Matucci R, Quaglia W.

Eur J Med Chem. 2017 Jan 5;125:233-244. doi: 10.1016/j.ejmech.2016.09.026. Epub 2016 Sep 9.

PMID:
27662034
14.

A Novel Class of Dopamine D4 Receptor Ligands Bearing an Imidazoline Nucleus.

Mammoli V, Bonifazi A, Dal Ben D, Giannella M, Giorgioni G, Piergentili A, Pigini M, Quaglia W, Thomas A, Newman AH, Ferré S, Sanchez-Soto M, Keck TM, Del Bello F.

ChemMedChem. 2016 Aug 19;11(16):1819-28. doi: 10.1002/cmdc.201600022. Epub 2016 Mar 15.

15.

Novel Potent N-Methyl-d-aspartate (NMDA) Receptor Antagonists or σ1 Receptor Ligands Based on Properly Substituted 1,4-Dioxane Ring.

Bonifazi A, Del Bello F, Mammoli V, Piergentili A, Petrelli R, Cimarelli C, Pellei M, Schepmann D, Wünsch B, Barocelli E, Bertoni S, Flammini L, Amantini C, Nabissi M, Santoni G, Vistoli G, Quaglia W.

J Med Chem. 2015 Nov 12;58(21):8601-15. doi: 10.1021/acs.jmedchem.5b01214. Epub 2015 Oct 14.

PMID:
26430967
16.

Identification of 2-aminopyrimidine derivatives as inhibitors of the canonical Wnt signaling pathway.

Del Bello F, Farande A, Giannella M, Piergentili A, Quaglia W, Benicchi T, Cappelli F, Nencini A, Salerno M, Thomas RJ, Travagli M, Varrone M.

Bioorg Med Chem. 2015 Sep 1;23(17):5725-33. doi: 10.1016/j.bmc.2015.07.015. Epub 2015 Jul 17.

PMID:
26233797
17.

Antagonism/Agonism modulation to build novel antihypertensives selectively triggering i1-imidazoline receptor activation.

Del Bello F, Bargelli V, Cifani C, Gratteri P, Bazzicalupi C, Diamanti E, Giannella M, Mammoli V, Matucci R, Micioni Di Bonaventura MV, Piergentili A, Quaglia W, Pigini M.

ACS Med Chem Lett. 2015 Apr 3;6(5):496-501. doi: 10.1021/acsmedchemlett.5b00115. eCollection 2015 May 14.

18.

Cross-talk between alpha1D-adrenoceptors and transient receptor potential vanilloid type 1 triggers prostate cancer cell proliferation.

Morelli MB, Amantini C, Nabissi M, Liberati S, Cardinali C, Farfariello V, Tomassoni D, Quaglia W, Piergentili A, Bonifazi A, Del Bello F, Santoni M, Mammana G, Servi L, Filosa A, Gismondi A, Santoni G.

BMC Cancer. 2014 Dec 7;14:921. doi: 10.1186/1471-2407-14-921.

19.

Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).

Bonifazi A, Yano H, Del Bello F, Farande A, Quaglia W, Petrelli R, Matucci R, Nesi M, Vistoli G, Ferré S, Piergentili A.

J Med Chem. 2014 Nov 13;57(21):9065-77. doi: 10.1021/jm501173q. Epub 2014 Oct 16.

PMID:
25275964
20.

Mode of interaction of 1,4-dioxane agonists at the M2 and M3 muscarinic receptor orthosteric sites.

Del Bello F, Bonifazi A, Quaglia W, Mazzolari A, Barocelli E, Bertoni S, Matucci R, Nesi M, Piergentili A, Vistoli G.

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3255-9. doi: 10.1016/j.bmcl.2014.06.020. Epub 2014 Jun 14.

PMID:
24980056
21.

Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.

Del Bello F, Diamanti E, Giannella M, Mammoli V, Mattioli L, Titomanlio F, Piergentili A, Quaglia W, Lanza M, Sabatini C, Caselli G, Poggesi E, Pigini M.

ACS Med Chem Lett. 2013 Jul 22;4(9):875-9. doi: 10.1021/ml400232p. eCollection 2013 Sep 12.

22.

GluN2B-selective N-methyl-D-aspartate (NMDA) receptor antagonists derived from 3-benzazepines: synthesis and pharmacological evaluation of benzo[7]annulen-7-amines.

Benner A, Bonifazi A, Shirataki C, Temme L, Schepmann D, Quaglia W, Shoji O, Watanabe Y, Daniliuc C, Wünsch B.

ChemMedChem. 2014 Apr;9(4):741-51. doi: 10.1002/cmdc.201300547. Epub 2014 Feb 23.

PMID:
24677663
23.

Structure-activity relationships in 1,4-benzodioxan-related compounds. 11. (1) reversed enantioselectivity of 1,4-dioxane derivatives in α1-adrenergic and 5-HT1A receptor binding sites recognition.

Bonifazi A, Piergentili A, Del Bello F, Farande Y, Giannella M, Pigini M, Amantini C, Nabissi M, Farfariello V, Santoni G, Poggesi E, Leonardi A, Menegon S, Quaglia W.

J Med Chem. 2013 Jan 24;56(2):584-8. doi: 10.1021/jm301525w. Epub 2013 Jan 8.

PMID:
23252794
24.

Roles of Wnt/β-catenin signalling pathway in the bony repair of injured growth plate cartilage in young rats.

Chung R, Wong D, Macsai C, Piergentili A, Del Bello F, Quaglia W, Xian CJ.

Bone. 2013 Feb;52(2):651-8. doi: 10.1016/j.bone.2012.10.035. Epub 2012 Nov 10.

PMID:
23149278
25.

Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.

Del Bello F, Diamanti E, Giannella M, Mammoli V, Marchioro C, Mattioli L, Titomanlio F, Piergentili A, Quaglia W, Benedetti G, Varrone M, Pigini M.

ACS Med Chem Lett. 2012 Jun 8;3(7):535-9. doi: 10.1021/ml300064v. eCollection 2012 Jul 12.

26.

Favourable involvement of α2A-adrenoreceptor antagonism in the I₂-imidazoline binding sites-mediated morphine analgesia enhancement.

Mammoli V, Bonifazi A, Del Bello F, Diamanti E, Giannella M, Hudson AL, Mattioli L, Perfumi M, Piergentili A, Quaglia W, Titomanlio F, Pigini M.

Bioorg Med Chem. 2012 Apr 1;20(7):2259-65. doi: 10.1016/j.bmc.2012.02.016. Epub 2012 Feb 13.

PMID:
22370341
27.

Might the observed α(2A)-adrenoreceptor agonism or antagonism of allyphenyline analogues be ascribed to different molecular conformations?

Diamanti E, Del Bello F, Carbonara G, Carrieri A, Fracchiolla G, Giannella M, Mammoli V, Piergentili A, Pohjanoksa K, Quaglia W, Scheinin M, Pigini M.

Bioorg Med Chem. 2012 Mar 15;20(6):2082-90. doi: 10.1016/j.bmc.2012.01.035. Epub 2012 Jan 31.

PMID:
22341244
28.

1,4-dioxane, a suitable scaffold for the development of novel M₃ muscarinic receptor antagonists.

Del Bello F, Barocelli E, Bertoni S, Bonifazi A, Camalli M, Campi G, Giannella M, Matucci R, Nesi M, Pigini M, Quaglia W, Piergentili A.

J Med Chem. 2012 Feb 23;55(4):1783-7. doi: 10.1021/jm2013216. Epub 2012 Feb 2.

PMID:
22243489
29.

α2C-adrenoceptor modulators: a patent review.

Quaglia W, Del Bello F, Giannella M, Piergentili A, Pigini M.

Expert Opin Ther Pat. 2011 Apr;21(4):455-81. doi: 10.1517/13543776.2011.565333. Review.

PMID:
21413828
30.

Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.

Del Bello F, Mattioli L, Ghelfi F, Giannella M, Piergentili A, Quaglia W, Cardinaletti C, Perfumi M, Thomas RJ, Zanelli U, Marchioro C, Dal Cin M, Pigini M.

J Med Chem. 2010 Nov 11;53(21):7825-35. doi: 10.1021/jm100977d.

PMID:
20925410
31.

Structure-activity relationships in 1,4-benzodioxan-related compounds. 10. Novel α1-adrenoreceptor antagonists related to openphendioxan: synthesis, biological evaluation, and α1d computational study.

Carrieri A, Piergentili A, Del Bello F, Giannella M, Pigini M, Leonardi A, Fanelli F, Quaglia W.

Bioorg Med Chem. 2010 Oct 1;18(19):7065-77. doi: 10.1016/j.bmc.2010.08.002. Epub 2010 Aug 6.

PMID:
20801662
32.

Novel highly potent and selective sigma 1 receptor antagonists related to spipethiane.

Piergentili A, Amantini C, Del Bello F, Giannella M, Mattioli L, Palmery M, Perfumi M, Pigini M, Santoni G, Tucci P, Zotti M, Quaglia W.

J Med Chem. 2010 Feb 11;53(3):1261-9. doi: 10.1021/jm901542q.

PMID:
20067271
33.

Properly substituted 1,4-dioxane nucleus favours the selective M3 muscarinic receptor activation.

Piergentili A, Quaglia W, Del Bello F, Giannella M, Pigini M, Barocelli E, Bertoni S, Matucci R, Nesi M, Bruni B, Di Vaira M.

Bioorg Med Chem. 2009 Dec 15;17(24):8174-85. doi: 10.1016/j.bmc.2009.10.027. Epub 2009 Oct 20.

PMID:
19896386
34.

Might adrenergic alpha2C-agonists/alpha2A-antagonists become novel therapeutic tools for pain treatment with morphine?

Cardinaletti C, Mattioli L, Ghelfi F, Del Bello F, Giannella M, Bruzzone A, Paris H, Perfumi M, Piergentili A, Quaglia W, Pigini M.

J Med Chem. 2009 Nov 26;52(22):7319-22. doi: 10.1021/jm901262f.

PMID:
19886609
35.

Structure-activity relationships in 1,4-benzodioxan-related compounds. 9. From 1,4-benzodioxane to 1,4-dioxane ring as a promising template of novel alpha1D-adrenoreceptor antagonists, 5-HT1A full agonists, and cytotoxic agents.

Quaglia W, Piergentili A, Del Bello F, Farande Y, Giannella M, Pigini M, Rafaiani G, Carrieri A, Amantini C, Lucciarini R, Santoni G, Poggesi E, Leonardi A.

J Med Chem. 2008 Oct 23;51(20):6359-70. doi: 10.1021/jm800461k. Epub 2008 Sep 26.

PMID:
18817363
36.

Dopamine D5 receptors: a challenge to medicinal chemists.

Giorgioni G, Piergentili A, Ruggieri S, Quaglia W.

Mini Rev Med Chem. 2008 Sep;8(10):976-95. Review.

PMID:
18782049
37.

Novel ligands rationally designed for characterizing I2-imidazoline binding sites nature and functions.

Gentili F, Cardinaletti C, Vesprini C, Ghelfi F, Farande A, Giannella M, Piergentili A, Quaglia W, Mattioli L, Perfumi M, Hudson A, Pigini M.

J Med Chem. 2008 Aug 28;51(16):5130-4. doi: 10.1021/jm800400k. Epub 2008 Jul 29.

PMID:
18661965
38.

Alpha2-adrenoreceptors profile modulation. 4. From antagonist to agonist behavior.

Gentili F, Cardinaletti C, Vesprini C, Carrieri A, Ghelfi F, Farande A, Giannella M, Piergentili A, Quaglia W, Laurila JM, Huhtinen A, Scheinin M, Pigini M.

J Med Chem. 2008 Jul 24;51(14):4289-99. doi: 10.1021/jm800250z. Epub 2008 Jun 25.

PMID:
18578476
39.

Rapid novel divergent synthesis and muscarinic agonist profile of all four optical isomers of N,N,N-trimethyl(6-methyl-1,4-dioxan-2-yl)methanaminium iodide.

Piergentili A, Quaglia W, Giannella M, Del Bello F, Buccioni M, Nesi M, Matucci R.

Bioorg Med Chem Lett. 2008 Jan 15;18(2):614-8. Epub 2007 Nov 28.

PMID:
18077164
40.

Alpha2-adrenoreceptors profile modulation. 3.1 (R)-(+)-m-nitrobiphenyline, a new efficient and alpha2C-subtype selective agonist.

Crassous PA, Cardinaletti C, Carrieri A, Bruni B, Di Vaira M, Gentili F, Ghelfi F, Giannella M, Paris H, Piergentili A, Quaglia W, Schaak S, Vesprini C, Pigini M.

J Med Chem. 2007 Aug 9;50(16):3964-8. Epub 2007 Jul 14.

PMID:
17630725
41.

Dioxane and oxathiane nuclei: suitable substructures for muscarinic agonists.

Piergentili A, Quaglia W, Giannella M, Del Bello F, Bruni B, Buccioni M, Carrieri A, Ciattini S.

Bioorg Med Chem. 2007 Jan 15;15(2):886-96. Epub 2006 Oct 21.

PMID:
17084634
42.
43.

alpha 2-adrenoreceptors profile modulation. 2. Biphenyline analogues as tools for selective activation of the alpha 2C-subtype.

Gentili F, Ghelfi F, Giannella M, Piergentili A, Pigini M, Quaglia W, Vesprini C, Crassous PA, Paris H, Carrieri A.

J Med Chem. 2004 Dec 2;47(25):6160-73.

PMID:
15566287
44.

I1 imidazoline receptor-mediated effects on apoptotic processes in PC12 cells.

Dupuy L, Urosevic D, Greney H, Quaglia W, Pigini M, Brasili L, Dontenwill M, Bousquet P.

Cell Death Differ. 2004 Sep;11(9):1049-52. No abstract available.

45.

Muscarinic subtypes profile modulation within a series of new antagonists, bridged bicyclic derivatives of 2,2-diphenyl-[1,3]-dioxolan-4-ylmethyl-dimethylamine.

Piergentili A, Gentili F, Ghelfi F, Marucci G, Pigini M, Quaglia W, Giannella M.

Bioorg Med Chem. 2003 Sep 1;11(18):3901-11.

PMID:
12927850
46.

Imidazoline binding sites (IBS) profile modulation: key role of the bridge in determining I1-IBS or I2-IBS selectivity within a series of 2-phenoxymethylimidazoline analogues.

Gentili F, Bousquet P, Brasili L, Dontenwill M, Feldman J, Ghelfi F, Giannella M, Piergentili A, Quaglia W, Pigini M.

J Med Chem. 2003 May 22;46(11):2169-76.

PMID:
12747788
47.

Binding of nicotine and homoazanicotine analogues at neuronal nicotinic acetylcholinergic (nACh) receptors.

Ferretti G, Dukat M, Giannella M, Piergentili A, Pigini M, Quaglia W, Damaj MI, Martin BR, Glennon RA.

Bioorg Med Chem Lett. 2003 Feb 24;13(4):733-5.

PMID:
12639569
48.

Homoazanicotine: a structure-affinity study for nicotinic acetylcholine (nACh) receptor binding.

Ferretti G, Dukat M, Giannella M, Piergentili A, Pigini M, Quaglia W, Damaj MI, Martin BR, Glennon RA.

J Med Chem. 2002 Oct 10;45(21):4724-31.

PMID:
12361399
49.

Structure-activity relationships in 1,4-benzodioxan-related compounds. 7. Selectivity of 4-phenylchroman analogues for alpha(1)-adrenoreceptor subtypes.

Quaglia W, Pigini M, Piergentili A, Giannella M, Gentili F, Marucci G, Carrieri A, Carotti A, Poggesi E, Leonardi A, Melchiorre C.

J Med Chem. 2002 Apr 11;45(8):1633-43.

PMID:
11931617
50.

Deoxamuscaroneoxime derivatives as useful muscarinic agonists to explore the muscarinic subsite: demox, a modulator of orthosteric and allosteric sites at cardiac muscarinic M2 receptors.

Angeli P, Marucci G, Buccioni M, Piergentili A, Giannella M, Quaglia W, Pigini M, Cantalamessa F, Nasuti C, Novi F, Maggio R, Qasem AR, Spampinato S.

Life Sci. 2002 Feb 8;70(12):1427-46.

PMID:
11883718

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