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Lead Optimization to Advance Protease-Activated Receptor-1 Antagonists in Early Discovery.
Mandal M, Madeira M, Amin RP, Buevich AV, Cheng A, Labroli M, Liu X, Acton J, Pio B, Basso A, Chobanian H, Dong G, Dropinski J, Guo Y, Guo Z, Kurowski S, Korfmacher W, Lee S, Meng D, Ondeyka D, Yang Z, Zhang R, Wei H, Wu Z, Zhang F, Wollenberg G, Biftu T, Greenlee WJ, Chintala M, Maletic M, Zhu Z. Mandal M, et al. Among authors: zhu z. J Med Chem. 2022 Apr 14;65(7):5575-5592. doi: 10.1021/acs.jmedchem.1c02048. Epub 2022 Mar 29. J Med Chem. 2022. PMID: 35349275
Generation of Leads for γ-Secretase Modulation.
Mandal M, Buevich A, Caldwell JP, Hyde L, Huang X, Liu X, McKittrick B, Mazzola RD, Pissarnitski D, Palani A, Zhang L, Parker E, Xiao L, Rindgen D, Zhu Z. Mandal M, et al. Among authors: zhu z. J Med Chem. 2020 Aug 13;63(15):8216-8230. doi: 10.1021/acs.jmedchem.0c00446. Epub 2020 Aug 4. J Med Chem. 2020. PMID: 32786237
Design and validation of bicyclic iminopyrimidinones as beta amyloid cleaving enzyme-1 (BACE1) inhibitors: conformational constraint to favor a bioactive conformation.
Mandal M, Zhu Z, Cumming JN, Liu X, Strickland C, Mazzola RD, Caldwell JP, Leach P, Grzelak M, Hyde L, Zhang Q, Terracina G, Zhang L, Chen X, Kuvelkar R, Kennedy ME, Favreau L, Cox K, Orth P, Buevich A, Voigt J, Wang H, Kazakevich I, McKittrick BA, Greenlee W, Parker EM, Stamford AW. Mandal M, et al. Among authors: zhu z. J Med Chem. 2012 Nov 8;55(21):9331-45. doi: 10.1021/jm301039c. Epub 2012 Oct 1. J Med Chem. 2012. PMID: 22989333
Structure-Based Design of an Iminoheterocyclic β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman Primates.
Mandal M, Wu Y, Misiaszek J, Li G, Buevich A, Caldwell JP, Liu X, Mazzola RD, Orth P, Strickland C, Voigt J, Wang H, Zhu Z, Chen X, Grzelak M, Hyde LA, Kuvelkar R, Leach PT, Terracina G, Zhang L, Zhang Q, Michener MS, Smith B, Cox K, Grotz D, Favreau L, Mitra K, Kazakevich I, McKittrick BA, Greenlee W, Kennedy ME, Parker EM, Cumming JN, Stamford AW. Mandal M, et al. Among authors: zhu z. J Med Chem. 2016 Apr 14;59(7):3231-48. doi: 10.1021/acs.jmedchem.5b01995. Epub 2016 Mar 22. J Med Chem. 2016. PMID: 26937601
Overcoming Time-Dependent Inhibition (TDI) of Cytochrome P450 3A4 (CYP3A4) Resulting from Bioactivation of a Fluoropyrimidine Moiety.
Mandal M, Mitra K, Grotz D, Lin X, Palamanda J, Kumari P, Buevich A, Caldwell JP, Chen X, Cox K, Favreau L, Hyde L, Kennedy ME, Kuvelkar R, Liu X, Mazzola RD, Parker E, Rindgen D, Sherer E, Wang H, Zhu Z, Stamford AW, Cumming JN. Mandal M, et al. Among authors: zhu z. J Med Chem. 2018 Dec 13;61(23):10700-10708. doi: 10.1021/acs.jmedchem.8b01326. Epub 2018 Nov 15. J Med Chem. 2018. PMID: 30388368
Synthesis and SAR Studies of Fused Oxadiazines as γ-Secretase Modulators for Treatment of Alzheimer's Disease.
Huang X, Zhou W, Liu X, Li H, Sun G, Mandal M, Vicarel M, Zhu X, Bennett C, McCraken T, Pissarnitski D, Zhao Z, Cole D, Gallo G, Zhu Z, Palani A, Aslanian R, Clader J, Czarniecki M, Greenlee W, Burnett D, Cohen-Williams M, Hyde L, Song L, Zhang L, Chu I, Buevich A. Huang X, et al. Among authors: zhu x, zhu z. ACS Med Chem Lett. 2012 Sep 4;3(11):931-5. doi: 10.1021/ml300209g. eCollection 2012 Nov 8. ACS Med Chem Lett. 2012. PMID: 24900409 Free PMC article.
Discovery of a Tetrahydrobenzisoxazole Series of γ-Secretase Modulators.
Zhao Z, Pissarnitski DA, Huang X, Palani A, Zhu Z, Greenlee WJ, Hyde LA, Song L, Terracina G, Zhang L, Parker EM. Zhao Z, et al. Among authors: zhu z. ACS Med Chem Lett. 2017 Sep 19;8(10):1002-1006. doi: 10.1021/acsmedchemlett.7b00178. eCollection 2017 Oct 12. ACS Med Chem Lett. 2017. PMID: 29057041 Free PMC article.
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