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Items: 1 to 50 of 83

1.

1,3-Dioxane as a scaffold for potent and selective 5-HT1AR agonist with in-vivo anxiolytic, anti-depressant and anti-nociceptive activity.

Franchini S, Sorbi C, Linciano P, Carnevale G, Tait A, Ronsisvalle S, Buccioni M, Del Bello F, Cilia A, Pirona L, Denora N, Iacobazzi RM, Brasili L.

Eur J Med Chem. 2019 Aug 15;176:310-325. doi: 10.1016/j.ejmech.2019.05.024. Epub 2019 May 11.

PMID:
31112892
2.

Weaning of Children With Burn Injury by Noninvasive Ventilation: A Clinical Experience.

Piastra M, Picconi E, Morena TC, Brasili L, Pizza A, Luca E, Tortorolo L, De Luca D, Cati G, Conti G, De Bellis A.

J Burn Care Res. 2019 Aug 14;40(5):689-695. doi: 10.1093/jbcr/irz068.

PMID:
31032522
3.

Effect of the rigidification of propranolol, a mixed β-adrenoceptor and 5-HT1AR antagonist.

Franchini S, Sorbi C, Linciano P, Brasili L, Tait A.

Pharmazie. 2019 Mar 1;74(3):131-135. doi: 10.1691/ph.2019.8878.

PMID:
30961676
4.

Synthesis and biological evaluation of 1,3-dioxolane-based 5-HT1A receptor agonists for CNS disorders and neuropathic pain.

Franchini S, Bencheva LI, Battisti UM, Tait A, Sorbi C, Fossa P, Cichero E, Ronsisvalle S, Aricò G, Denora N, Iacobazzi RM, Cilia A, Pirona L, Brasili L.

Future Med Chem. 2018 Sep 1;10(18):2137-2154. doi: 10.4155/fmc-2018-0107. Epub 2018 Jul 25.

PMID:
30043643
5.

Structure-Activity Relationships within a Series of σ1 and σ2 Receptor Ligands: Identification of a σ2 Receptor Agonist (BS148) with Selective Toxicity against Metastatic Melanoma.

Franchini S, Sorbi C, Battisti UM, Tait A, Bencheva LI, Cichero E, Fossa P, Cilia A, Prezzavento O, Ronsisvalle S, Aricò G, Benassi L, Vaschieri C, Azzoni P, Magnoni C, Brasili L.

ChemMedChem. 2017 Nov 22;12(22):1893-1905. doi: 10.1002/cmdc.201700427. Epub 2017 Oct 30.

PMID:
28940806
6.

Exhaustive CoMFA and CoMSIA analyses around different chemical entities: a ligand-based study exploring the affinity and selectivity profiles of 5-HT1A ligands.

Guariento S, Franchini S, Tonelli M, Fossa P, Sorbi C, Cichero E, Brasili L.

J Enzyme Inhib Med Chem. 2017 Dec;32(1):214-230. doi: 10.1080/14756366.2016.1247057.

7.

Synthesis, biological evaluation and molecular modeling of 1-oxa-4-thiaspiro- and 1,4-dithiaspiro[4.5]decane derivatives as potent and selective 5-HT1A receptor agonists.

Franchini S, Manasieva LI, Sorbi C, Battisti UM, Fossa P, Cichero E, Denora N, Iacobazzi RM, Cilia A, Pirona L, Ronsisvalle S, Aricò G, Brasili L.

Eur J Med Chem. 2017 Jan 5;125:435-452. doi: 10.1016/j.ejmech.2016.09.050. Epub 2016 Sep 17.

PMID:
27689727
8.

Synthesis, structural characterization and biological evaluation of 4'-C-methyl- and phenyl-dioxolane pyrimidine and purine nucleosides.

Franchini S, Battisti UM, Sorbi C, Tait A, Cornia A, Jeong LS, Lee SK, Song J, Loddo R, Madeddu S, Sanna G, Brasili L.

Arch Pharm Res. 2017 May;40(5):537-549. doi: 10.1007/s12272-016-0825-6. Epub 2016 Sep 11.

PMID:
27615010
9.

Scouting new sigma receptor ligands: Synthesis, pharmacological evaluation and molecular modeling of 1,3-dioxolane-based structures and derivatives.

Franchini S, Battisti UM, Prandi A, Tait A, Borsari C, Cichero E, Fossa P, Cilia A, Prezzavento O, Ronsisvalle S, Aricò G, Parenti C, Brasili L.

Eur J Med Chem. 2016 Apr 13;112:1-19. doi: 10.1016/j.ejmech.2016.01.059. Epub 2016 Feb 1.

PMID:
26874044
10.

Synthesis and Structure-Activity Relationships of Triazaspirodecanone Derivatives as Nociceptin/Orphanin FQ Receptor Ligands.

Corrado S, Battisti UM, Sorbi C, Tait A, Malfacini D, Camarda V, Calò G, Brasili L.

Chem Biol Drug Des. 2015 Oct;86(4):447-58. doi: 10.1111/cbdd.12505. Epub 2015 Jan 20.

PMID:
25546401
11.

Structure-affinity/activity relationships of 1,4-dioxa-spiro[4.5]decane based ligands at α<alpha>1 and 5-HT1A receptors.

Franchini S, Battisti UM, Baraldi A, Prandi A, Fossa P, Cichero E, Tait A, Sorbi C, Marucci G, Cilia A, Pirona L, Brasili L.

Eur J Med Chem. 2014 Nov 24;87:248-66. doi: 10.1016/j.ejmech.2014.09.070. Epub 2014 Sep 27.

PMID:
25261823
12.

Further insights into the pharmacology of the human trace amine-associated receptors: discovery of novel ligands for TAAR1 by a virtual screening approach.

Cichero E, Espinoza S, Franchini S, Guariento S, Brasili L, Gainetdinov RR, Fossa P.

Chem Biol Drug Des. 2014 Dec;84(6):712-20. doi: 10.1111/cbdd.12367. Epub 2014 Jun 30.

PMID:
24894156
13.

Oropharyngeal exercises to reduce symptoms of OSA after AT.

Villa MP, Brasili L, Ferretti A, Vitelli O, Rabasco J, Mazzotta AR, Pietropaoli N, Martella S.

Sleep Breath. 2015 Mar;19(1):281-9. doi: 10.1007/s11325-014-1011-z. Epub 2014 May 26.

PMID:
24859614
14.
15.

Insights into the structure and pharmacology of the human trace amine-associated receptor 1 (hTAAR1): homology modelling and docking studies.

Cichero E, Espinoza S, Gainetdinov RR, Brasili L, Fossa P.

Chem Biol Drug Des. 2013 Apr;81(4):509-16. doi: 10.1111/cbdd.12018.

PMID:
22883051
16.

Synthesis of 5-methyl-1,3-oxathiolane-based nucleoside analogues as potential antiviral agents.

Franchini S, Tait A, Sorbi C, Brasili L.

Med Chem. 2012 Sep;8(5):769-78.

PMID:
22741790
17.

5-Arylbenzothiadiazine Type Compounds as Positive Allosteric Modulators of AMPA/Kainate Receptors.

Battisti UM, Jozwiak K, Cannazza G, Puia G, Stocca G, Braghiroli D, Parenti C, Brasili L, Carrozzo MM, Citti C, Troisi L.

ACS Med Chem Lett. 2011 Nov 14;3(1):25-9. doi: 10.1021/ml200184w. eCollection 2012 Jan 12.

18.

Synthesis, biological evaluation, and docking studies of tetrahydrofuran- cyclopentanone- and cyclopentanol-based ligands acting at adrenergic α₁- and serotonine 5-HT1A receptors.

Prandi A, Franchini S, Manasieva LI, Fossa P, Cichero E, Marucci G, Buccioni M, Cilia A, Pirona L, Brasili L.

J Med Chem. 2012 Jan 12;55(1):23-36. doi: 10.1021/jm200421e. Epub 2011 Dec 22.

PMID:
22145629
19.

Evaluation of stereo and chemical stability of chiral compounds.

Cannazza G, Battisti U, Carrozzo MM, Brasili L, Braghiroli D, Parenti C.

Chirality. 2011 Nov;23(10):851-9. doi: 10.1002/chir.20941. Epub 2011 Sep 20.

PMID:
21932212
20.

1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors.

Franchini S, Prandi A, Baraldi A, Sorbi C, Tait A, Buccioni M, Marucci G, Cilia A, Pirona L, Fossa P, Cichero E, Brasili L.

Eur J Med Chem. 2010 Sep;45(9):3740-51. doi: 10.1016/j.ejmech.2010.05.023. Epub 2010 May 15.

PMID:
20605276
21.

Discovery of a new series of 5-HT1A receptor agonists.

Franchini S, Prandi A, Sorbi C, Tait A, Baraldi A, Angeli P, Buccioni M, Cilia A, Poggesi E, Fossa P, Brasili L.

Bioorg Med Chem Lett. 2010 Mar 15;20(6):2017-20. doi: 10.1016/j.bmcl.2010.01.030. Epub 2010 Feb 4.

PMID:
20185311
22.

The XIXth National Meeting on Medicinal Chemistry: Verona, Italy.

Brasili L, Donati D, Mosti L.

ChemMedChem. 2009 Jun;4(6):899-904. doi: 10.1002/cmdc.200900168.

PMID:
19479883
23.

1,3-Dioxolane-based ligands as rigid analogues of naftopidil: structure-affinity/activity relationships at alpha1 and 5-HT1A receptors.

Sorbi C, Franchini S, Tait A, Prandi A, Gallesi R, Angeli P, Marucci G, Pirona L, Poggesi E, Brasili L.

ChemMedChem. 2009 Mar;4(3):393-9. doi: 10.1002/cmdc.200800277.

PMID:
19152363
24.

(2,2-Diphenyl-[1,3]oxathiolan-5-ylmethyl)-(3-phenyl-propyl)-amine: a potent and selective 5-HT(1A) receptor agonist.

Franchini S, Tait A, Prandi A, Sorbi C, Gallesi R, Buccioni M, Marucci G, De Stefani C, Cilia A, Brasili L.

ChemMedChem. 2009 Feb;4(2):196-203. doi: 10.1002/cmdc.200800276.

PMID:
19101959
25.

1,2,4-Benzothiadiazine derivatives as alpha1 and 5-HT1A receptor ligands.

Tait A, Luppi A, Franchini S, Preziosi E, Parenti C, Buccioni M, Marucci G, Leonardi A, Poggesi E, Brasili L.

Bioorg Med Chem Lett. 2005 Feb 15;15(4):1185-8.

PMID:
15686938
26.

Synthesis and structure-activity relationships of 1-aralkyl-4-benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent sigma ligands.

Costantino L, Gandolfi F, Sorbi C, Franchini S, Prezzavento O, Vittorio F, Ronsisvalle G, Leonardi A, Poggesi E, Brasili L.

J Med Chem. 2005 Jan 13;48(1):266-73.

PMID:
15634021
27.

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.

28.

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
29.

1,3-dioxolane-based ligands as a novel class of alpha1-adrenoceptor antagonists.

Brasili L, Sorbi C, Franchini S, Manicardi M, Angeli P, Marucci G, Leonardi A, Poggesi E.

J Med Chem. 2003 Apr 10;46(8):1504-11.

PMID:
12672251
30.

Alpha2-adrenoreceptors profile modulation and high antinociceptive activity of (S)-(-)-2-[1-(biphenyl-2-yloxy)ethyl]-4,5-dihydro-1H-imidazole.

Gentili F, Bousquet P, Brasili L, Caretto M, Carrieri A, Dontenwill M, Giannella M, Marucci G, Perfumi M, Piergentili A, Quaglia W, Rascente C, Pigini M.

J Med Chem. 2002 Jan 3;45(1):32-40.

PMID:
11754577
31.

Synthesis, absolute configuration and antimuscarinic activity of the enantiomers of [1-(2,2-diphenyl-[1,3]dioxolan-4-yl)-ethyl]-dimethyl-amine.

Gulini U, Angeli P, Marucci G, Buccioni M, Giardinà D, Antolini L, Franchini S, Sorbi C, Brasili L.

Bioorg Med Chem Lett. 2001 Jan 22;11(2):247-50.

PMID:
11206470
32.

Structure-activity relationship at alpha-adrenergic receptors within a series of imidazoline analogues of cirazoline.

Pigini M, Quaglia W, Gentili F, Marucci G, Cantalamessa F, Franchini S, Sorbi C, Brasili L.

Bioorg Med Chem. 2000 May;8(5):883-8.

PMID:
10882000
33.

Coupling of I(1) imidazoline receptors to the cAMP pathway: studies with a highly selective ligand, benazoline.

Greney H, Ronde P, Magnier C, Maranca F, Rascente C, Quaglia W, Giannella M, Pigini M, Brasili L, Lugnier C, Bousquet P, Dontenwill M.

Mol Pharmacol. 2000 Jun;57(6):1142-51.

PMID:
10825384
34.

Enigmatic receptors.

Brasili L.

Pharm Acta Helv. 2000 Mar;74(2-3):201-3. Review.

PMID:
10812958
35.

2-(2-Phenylcyclopropyl)imidazolines: reversed enantioselective interaction at I(1) and I(2) imidazoline receptors.

Quaglia W, Bousquet P, Pigini M, Carotti A, Carrieri A, Dontenwill M, Gentili F, Giannella M, Maranca F, Piergentili A, Brasili L.

J Med Chem. 1999 Jul 29;42(15):2737-40. No abstract available.

PMID:
10425083
36.

Binding of tracizolines to the imidazoline receptor. Role of lipophilicity in quantitative structure-activity relationship models.

Pigini M, Bousquet P, Brasili L, Carrieri A, Dontenwill M, Gentili F, Giannella M, Leonetti F, Piergentili A, Quaglia W, Carotti A.

Ann N Y Acad Sci. 1999 Jun 21;881:118-22. No abstract available.

PMID:
10415907
37.

An unexpected central hypertensive effect of the new imidazoline compound benazoline.

Bruban V, Feldman J, Dontenwill M, Greney H, Brasili L, Giannella M, Pigini M, Bousquet P.

Ann N Y Acad Sci. 1999 Jun 21;881:102-5. No abstract available.

PMID:
10415903
38.

Ligand binding to I2 imidazoline receptor: the role of lipophilicity in quantitative structure-activity relationship models.

Pigini M, Bousquet P, Brasili L, Carrieri A, Cavagna R, Dontenwill M, Gentili F, Giannella M, Leonetti F, Piergentili A, Quaglia W, Carotti A.

Bioorg Med Chem. 1998 Dec;6(12):2245-60.

PMID:
9925287
39.

Synthesis and antimuscarinic activity of some ether- and thioether-bearing 1,3-dioxolanes and related sulfoxides and sulfones.

Malmusi L, Franchini S, Mucci A, Schenetti L, Gulini U, Marucci G, Brasili L.

Bioorg Med Chem. 1998 Jun;6(6):825-32.

PMID:
9681148
40.

1'-Benzyl-3,4-dihydrospiro[2H-1- benzothiopyran-2,4'-piperidine] (spipethiane), a potent and highly selective sigma1 ligand.

Quaglia W, Giannella M, Piergentili A, Pigini M, Brasili L, Di Toro R, Rossetti L, Spampinato S, Melchiorre C.

J Med Chem. 1998 May 7;41(10):1557-60. No abstract available.

PMID:
9572880
41.

2-D and 3-D modeling of imidazoline receptor ligands: insights into pharmacophore.

Carrieri A, Brasili L, Leonetti F, Pigini M, Giannella M, Bousquet P, Carotti A.

Bioorg Med Chem. 1997 May;5(5):843-56.

PMID:
9208096
42.

Imidazoline receptors: qualitative structure-activity relationships and discovery of tracizoline and benazoline. Two ligands with high affinity and unprecedented selectivity.

Pigini M, Bousquet P, Carotti A, Dontenwill M, Giannella M, Moriconi R, Piergentili A, Quaglia W, Tayebati SK, Brasili L.

Bioorg Med Chem. 1997 May;5(5):833-41.

PMID:
9208095
43.

Synthesis and structure-activity relationship studies in a series of 2-substituted 1,3-dioxolanes modified at the cationic head.

Angeli P, Brasili L, Cingolani ML, Marucci G, Piergentili A, Pigini M, Quaglia W.

Bioorg Med Chem. 1997 Apr;5(4):731-7.

PMID:
9158872
44.

Synthesis, NMR spectroscopy study, and antimuscarinic activity of a series of 2-(acyloxymethyl)-1,3-dioxolanes.

Malmusi L, Mucci A, Schenetti L, Gulini U, Marucci G, Brasili L.

Bioorg Med Chem. 1996 Dec;4(12):2071-80.

PMID:
9022972
45.

Separation of alpha-adrenergic and imidazoline/guanidinium receptive sites (IGRS) activity in a series of imidazoline analogues of cirazoline.

Brasili L, Pigini M, Marucci G, Quaglia W, Malmusi L, Lanier SM, Lanier B.

Bioorg Med Chem. 1995 Nov;3(11):1503-9.

PMID:
8634830
46.

Structure-affinity relationship of cirazoline derivatives for idazoxan imidazoline-specific sites in the human cerebral cortex and the rabbit kidney.

Brasili L, Pigini M, Ehrhardt JD, Molines A, Greney H, Bousquet P, Dontenwill M.

Ann N Y Acad Sci. 1995 Jul 12;763:149-52. No abstract available.

PMID:
7677323
47.

Synthesis and muscarinic receptors affinity of a series of antagonist bivalent ligands.

Piergentili A, Quaglia W, Tayebati SK, Paparelli F, Malmusi L, Brasili L.

Farmaco. 1994 Feb;49(2):83-7.

PMID:
7516166
48.

Pharmacological characterization of muscarinic receptor subtypes in rabbit isolated tissue preparations.

Angeli P, Brasili L, Cingolani ML, Marucci G, Pigini P, Tonnini MC.

J Auton Pharmacol. 1991 Oct;11(5):315-21.

PMID:
1748691
49.

Determination of muscarinic agonist potencies at M1 and M2 muscarinic receptors in a modified pithed rat preparation.

Angeli P, Brasili L, Cantalamessa F, Marucci G, Wess J.

Naunyn Schmiedebergs Arch Pharmacol. 1990 Dec;342(6):625-9.

PMID:
2096296
50.

Synthesis and Ca-antagonist activity of some benzhydryl derivatives.

Corsano S, Strappaghetti G, Di Domenico E, Brasili L, Picchio MT.

Arch Pharm (Weinheim). 1989 Dec;322(12):873-8.

PMID:
2619516

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