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Items: 1 to 20 of 36

1.

Synthesis, Docking and Biological Evaluation of a Novel Class of Imidazothiazoles as IDO1 Inhibitors.

Serafini M, Torre E, Aprile S, Massarotti A, Fallarini S, Pirali T.

Molecules. 2019 May 15;24(10). pii: E1874. doi: 10.3390/molecules24101874.

2.

Drug Discovery for Soft Drugs on TRPV1 and TRPM8 Channels Using the Passerini Reaction.

Pirali T, Galli U, Serafini M, Griglio A, Genazzani AA, Tron GC.

Methods Mol Biol. 2019;1987:207-221. doi: 10.1007/978-1-4939-9446-5_13.

PMID:
31028682
3.

Applications of Deuterium in Medicinal Chemistry.

Pirali T, Serafini M, Cargnin S, Genazzani AA.

J Med Chem. 2019 Jun 13;62(11):5276-5297. doi: 10.1021/acs.jmedchem.8b01808. Epub 2019 Jan 25.

PMID:
30640460
4.

Inhalation of the prodrug PI3K inhibitor CL27c improves lung function in asthma and fibrosis.

Campa CC, Silva RL, Margaria JP, Pirali T, Mattos MS, Kraemer LR, Reis DC, Grosa G, Copperi F, Dalmarco EM, Lima-Júnior RCP, Aprile S, Sala V, Dal Bello F, Prado DS, Alves-Filho JC, Medana C, Cassali GD, Tron GC, Teixeira MM, Ciraolo E, Russo RC, Hirsch E.

Nat Commun. 2018 Dec 12;9(1):5232. doi: 10.1038/s41467-018-07698-6.

5.

Arynes and isocyanides: Two close-knit partners in multicomponent reactions.

Serafini M, Pirali T.

Drug Discov Today Technol. 2018 Nov;29:35-41. doi: 10.1016/j.ddtec.2018.06.007. Epub 2018 Jul 2. Review.

PMID:
30471672
6.

Pyrtriazoles, a Novel Class of Store-Operated Calcium Entry Modulators: Discovery, Biological Profiling, and in Vivo Proof-of-Concept Efficacy in Acute Pancreatitis.

Riva B, Griglio A, Serafini M, Cordero-Sanchez C, Aprile S, Di Paola R, Gugliandolo E, Alansary D, Biocotino I, Lim D, Grosa G, Galli U, Niemeyer B, Sorba G, Canonico PL, Cuzzocrea S, Genazzani AA, Pirali T.

J Med Chem. 2018 Nov 8;61(21):9756-9783. doi: 10.1021/acs.jmedchem.8b01512. Epub 2018 Oct 30.

PMID:
30347159
7.

Targeting Transient Receptor Potential Vanilloid 1 (TRPV1) Channel Softly: The Discovery of Passerini Adducts as a Topical Treatment for Inflammatory Skin Disorders.

Serafini M, Griglio A, Aprile S, Seiti F, Travelli C, Pattarino F, Grosa G, Sorba G, Genazzani AA, Gonzalez-Rodriguez S, Butron L, Devesa I, Fernandez-Carvajal A, Pirali T, Ferrer-Montiel A.

J Med Chem. 2018 May 24;61(10):4436-4455. doi: 10.1021/acs.jmedchem.8b00109. Epub 2018 May 15.

PMID:
29722529
8.

A multicomponent approach in the discovery of indoleamine 2,3-dioxygenase 1 inhibitors: Synthesis, biological investigation and docking studies.

Griglio A, Torre E, Serafini M, Bianchi A, Schmid R, Coda Zabetta G, Massarotti A, Sorba G, Pirali T, Fallarini S.

Bioorg Med Chem Lett. 2018 Feb 15;28(4):651-657. doi: 10.1016/j.bmcl.2018.01.032. Epub 2018 Feb 2.

PMID:
29398544
9.

Identification of a Potent Phosphoinositide 3-Kinase Pan Inhibitor Displaying a Strategic Carboxylic Acid Group and Development of Its Prodrugs.

Pirali T, Ciraolo E, Aprile S, Massarotti A, Berndt A, Griglio A, Serafini M, Mercalli V, Landoni C, Campa CC, Margaria JP, Silva RL, Grosa G, Sorba G, Williams R, Hirsch E, Tron GC.

ChemMedChem. 2017 Sep 21;12(18):1542-1554. doi: 10.1002/cmdc.201700340. Epub 2017 Aug 31.

10.

An aryne-based three-component access to α-aroylamino amides.

Serafini M, Griglio A, Viarengo S, Aprile S, Pirali T.

Org Biomol Chem. 2017 Aug 9;15(31):6604-6612. doi: 10.1039/c7ob01715d.

PMID:
28752162
11.

Transition-Metal-Free Synthesis of 2-Arylimidazolones via Cascade Reaction between Arynes and α,α'-Disubstituted α-Isocyanoacetamides.

Gesù A, Pozzoli C, Torre E, Aprile S, Pirali T.

Org Lett. 2016 May 6;18(9):1992-5. doi: 10.1021/acs.orglett.6b00580. Epub 2016 Apr 8.

PMID:
27057924
12.

A concise synthesis of pyrazole analogues of combretastatin A1 as potent anti-tubulin agents.

Zaninetti R, Cortese SV, Aprile S, Massarotti A, Canonico PL, Sorba G, Grosa G, Genazzani AA, Pirali T.

ChemMedChem. 2013 Apr;8(4):633-43. doi: 10.1002/cmdc.201200561. Epub 2013 Feb 21.

PMID:
23436706
13.

Transition-metal-free direct arylation of anilines.

Pirali T, Zhang F, Miller AH, Head JL, McAusland D, Greaney MF.

Angew Chem Int Ed Engl. 2012 Jan 23;51(4):1006-9. doi: 10.1002/anie.201106150. Epub 2011 Dec 12. No abstract available.

PMID:
22162111
14.

Regioselective Suzuki coupling of dihaloheteroaromatic compounds as a rapid strategy to synthesize potent rigid combretastatin analogues.

Theeramunkong S, Caldarelli A, Massarotti A, Aprile S, Caprioglio D, Zaninetti R, Teruggi A, Pirali T, Grosa G, Tron GC, Genazzani AA.

J Med Chem. 2011 Jul 28;54(14):4977-86. doi: 10.1021/jm200555r. Epub 2011 Jun 30.

PMID:
21696175
15.

Stereospecific synthesis of syn-α-oximinoamides by a three-component reaction of isocyanides, syn-chlorooximes, and carboxylic acids.

Pirali T, Mossetti R, Galli S, Tron GC.

Org Lett. 2011 Jul 15;13(14):3734-7. doi: 10.1021/ol201397x. Epub 2011 Jun 13.

PMID:
21667987
16.

Imides: forgotten players in the Ugi reaction. One-pot multicomponent synthesis of quinazolinones.

Mossetti R, Pirali T, Saggiorato D, Tron GC.

Chem Commun (Camb). 2011 Jun 28;47(24):6966-8. doi: 10.1039/c1cc12067k. Epub 2011 May 17.

PMID:
21589958
17.

Groebke multicomponent reaction and subsequent nucleophilic aromatic substitution for a convenient synthesis of 3,8-diaminoimidazo[1,2-a]pyrazines as potential kinase inhibitors.

Guasconi M, Lu X, Massarotti A, Caldarelli A, Ciraolo E, Tron GC, Hirsch E, Sorba G, Pirali T.

Org Biomol Chem. 2011 Jun 7;9(11):4144-9. doi: 10.1039/c1ob05336a. Epub 2011 Apr 14.

PMID:
21494711
18.

A novel α-isocyanoacetamide-based three-component reaction for the synthesis of dialkyl 2-acyl-5-aminofuran-3,4-dicarboxylates.

Mossetti R, Caprioglio D, Colombano G, Tron GC, Pirali T.

Org Biomol Chem. 2011 Mar 7;9(5):1627-31. doi: 10.1039/c0ob00979b. Epub 2011 Jan 20.

PMID:
21249262
19.

Replacement of the double bond of antitubulin chalcones with triazoles and tetrazoles: Synthesis and biological evaluation.

Mesenzani O, Massarotti A, Giustiniano M, Pirali T, Bevilacqua V, Caldarelli A, Canonico P, Sorba G, Novellino E, Genazzani AA, Tron GC.

Bioorg Med Chem Lett. 2011 Jan 15;21(2):764-8. doi: 10.1016/j.bmcl.2010.11.113. Epub 2010 Nov 28.

PMID:
21167709
20.

Activation of TRPV4 channels reduces migration of immortalized neuroendocrine cells.

Zaninetti R, Fornarelli A, Ciarletta M, Lim D, Caldarelli A, Pirali T, Cariboni A, Owsianik G, Nilius B, Canonico PL, Distasi C, Genazzani AA.

J Neurochem. 2011 Feb;116(4):606-15. doi: 10.1111/j.1471-4159.2010.07144.x. Epub 2011 Jan 19.

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