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Page 1
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
Di Fabio R, Pellacani A, Faedo S, Roth A, Piccoli L, Gerrard P, Porter RA, Johnson CN, Thewlis K, Donati D, Stasi L, Spada S, Stemp G, Nash D, Branch C, Kindon L, Massagrande M, Poffe A, Braggio S, Chiarparin E, Marchioro C, Ratti E, Corsi M. Di Fabio R, et al. Among authors: stasi l. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5562-7. doi: 10.1016/j.bmcl.2011.06.086. Epub 2011 Jun 30. Bioorg Med Chem Lett. 2011. PMID: 21831639
Novel carbazole derivatives as NPY Y1 antagonists.
Leslie CP, Di Fabio R, Bonetti F, Borriello M, Braggio S, Dal Forno G, Donati D, Falchi A, Ghirlanda D, Giovannini R, Pavone F, Pecunioso A, Pentassuglia G, Pizzi DA, Rumboldt G, Stasi L. Leslie CP, et al. Among authors: stasi l. Bioorg Med Chem Lett. 2007 Feb 15;17(4):1043-6. doi: 10.1016/j.bmcl.2006.11.034. Epub 2006 Nov 16. Bioorg Med Chem Lett. 2007. PMID: 17127055
Discovery of 1-(3-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone (GSK163090), a Potent, selective, and orally active 5-HT1A/B/D receptor antagonist.
Leslie CP, Biagetti M, Bison S, Bromidge SM, Di Fabio R, Donati D, Falchi A, Garnier MJ, Jaxa-Chamiec A, Manchee G, Merlo G, Pizzi DA, Stasi LP, Tibasco J, Vong A, Ward SE, Zonzini L. Leslie CP, et al. Among authors: stasi lp. J Med Chem. 2010 Dec 9;53(23):8228-40. doi: 10.1021/jm100714c. Epub 2010 Nov 5. J Med Chem. 2010. PMID: 21053897
Novel spirotetracyclic zwitterionic dual H(1)/5-HT(2A) receptor antagonists for the treatment of sleep disorders.
Gianotti M, Botta M, Brough S, Carletti R, Castiglioni E, Corti C, Dal-Cin M, Delle Fratte S, Korajac D, Lovric M, Merlo G, Mesic M, Pavone F, Piccoli L, Rast S, Roscic M, Sava A, Smehil M, Stasi L, Togninelli A, Wigglesworth MJ. Gianotti M, et al. Among authors: stasi l. J Med Chem. 2010 Nov 11;53(21):7778-95. doi: 10.1021/jm100856p. J Med Chem. 2010. PMID: 20942472
6-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors.
Bromidge SM, Bertani B, Borriello M, Faedo S, Gordon LJ, Granci E, Hill M, Marshall HR, Stasi LP, Zucchelli V, Merlo G, Vesentini A, Watson JM, Zonzini L. Bromidge SM, et al. Among authors: stasi lp. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5653-6. doi: 10.1016/j.bmcl.2008.08.084. Epub 2008 Aug 28. Bioorg Med Chem Lett. 2008. PMID: 18799312
Discovery, synthesis, selectivity modulation and DMPK characterization of 5-azaspiro[2.4]heptanes as potent orexin receptor antagonists.
Stasi LP, Artusi R, Bovino C, Buzzi B, Canciani L, Caselli G, Colace F, Garofalo P, Giambuzzi S, Larger P, Letari O, Mandelli S, Perugini L, Pucci S, Salvi M, Toro P. Stasi LP, et al. Bioorg Med Chem Lett. 2013 May 1;23(9):2653-8. doi: 10.1016/j.bmcl.2013.02.093. Epub 2013 Mar 1. Bioorg Med Chem Lett. 2013. PMID: 23535328
Synthesis, pharmacophore modeling and in vitro activity of 10,11-dihydrodibenzo[b,f]oxepine-4-carboxamide derivatives as novel and potent antagonists of the prostaglandin EP4 receptor.
Stasi LP, Bhimani K, Borriello M, Canciani L, Caselli G, Colace F, Ferioli C, Kaswala M, Mennuni L, Piepoli T, Pucci S, Salvi M, Shirsath V, Zanelli T, Zerbi S. Stasi LP, et al. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6336-40. doi: 10.1016/j.bmcl.2011.08.102. Epub 2011 Sep 1. Bioorg Med Chem Lett. 2011. PMID: 21930381
Discovery of 5-substituent-N-arylbenzamide derivatives as potent, selective and orally bioavailable LRRK2 inhibitors.
Ding X, Dai X, Long K, Peng C, Andreotti D, Bamborough P, Eatherton AJ, Edge C, Jandu KS, Nichols PL, Philps OJ, Stasi LP, Wan Z, Xiang JN, Dong K, Dossang P, Ho MH, Li Y, Mensah L, Guan X, Reith AD, Ren F. Ding X, et al. Among authors: stasi lp. Bioorg Med Chem Lett. 2017 Sep 1;27(17):4034-4038. doi: 10.1016/j.bmcl.2017.07.052. Epub 2017 Jul 21. Bioorg Med Chem Lett. 2017. PMID: 28774425
137 results