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19 results

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Page 1
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 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 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. 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
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. J Med Chem. 2010 Nov 11;53(21):7778-95. doi: 10.1021/jm100856p. J Med Chem. 2010. PMID: 20942472
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. 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
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
Prostaglandin EP4 antagonists.
Borriello M, Stasi LP. Borriello M, et al. Among authors: stasi lp. Pharm Pat Anal. 2013 May;2(3):387-97. doi: 10.4155/ppa.13.15. Pharm Pat Anal. 2013. PMID: 24237064 Review.
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
5-Substituted-N-pyridazinylbenzamides as potent and selective LRRK2 inhibitors: Improved brain unbound fraction enables efficacy.
Ding X, Stasi LP, Dai X, Long K, Peng C, Zhao B, Wang H, Sun C, Hu H, Wan Z, Jandu KS, Philps OJ, Chen Y, Wang L, Liu Q, Edge C, Li Y, Dong K, Guan X, Tattersall FD, Reith AD, Ren F. Ding X, et al. Among authors: stasi lp. Bioorg Med Chem Lett. 2019 Jan 15;29(2):212-215. doi: 10.1016/j.bmcl.2018.11.054. Epub 2018 Nov 28. Bioorg Med Chem Lett. 2019. PMID: 30522952
19 results