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Page 1
Discovery and Optimization of Potent, Selective, and Brain-Penetrant 1-Heteroaryl-1H-Indazole LRRK2 Kinase Inhibitors for the Treatment of Parkinson's Disease.
Candito DA, Simov V, Gulati A, Kattar S, Chau RW, Lapointe BT, Methot JL, DeMong DE, Graham TH, Kurukulasuriya R, Keylor MH, Tong L, Morriello GJ, Acton JJ, Pio B, Liu W, Scott JD, Ardolino MJ, Martinot TA, Maddess ML, Yan X, Gunaydin H, Palte RL, McMinn SE, Nogle L, Yu H, Minnihan EC, Lesburg CA, Liu P, Su J, Hegde LG, Moy LY, Woodhouse JD, Faltus R, Xiong T, Ciaccio P, Piesvaux JA, Otte KM, Kennedy ME, Bennett DJ, DiMauro EF, Fell MJ, Neelamkavil S, Wood HB, Fuller PH, Ellis JM. Candito DA, et al. Among authors: morriello gj. J Med Chem. 2022 Dec 22;65(24):16801-16817. doi: 10.1021/acs.jmedchem.2c01605. Epub 2022 Dec 7. J Med Chem. 2022. PMID: 36475697
Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.
Edmondson SD, Zhu C, Kar NF, Di Salvo J, Nagabukuro H, Sacre-Salem B, Dingley K, Berger R, Goble SD, Morriello G, Harper B, Moyes CR, Shen DM, Wang L, Ball R, Fitzmaurice A, Frenkl T, Gichuru LN, Ha S, Hurley AL, Jochnowitz N, Levorse D, Mistry S, Miller RR, Ormes J, Salituro GM, Sanfiz A, Stevenson AS, Villa K, Zamlynny B, Green S, Struthers M, Weber AE. Edmondson SD, et al. J Med Chem. 2016 Jan 28;59(2):609-23. doi: 10.1021/acs.jmedchem.5b01372. Epub 2016 Jan 8. J Med Chem. 2016. PMID: 26709102
Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV-1 Protease Inhibitors.
Bungard CJ, Williams PD, Schulz J, Wiscount CM, Holloway MK, Loughran HM, Manikowski JJ, Su HP, Bennett DJ, Chang L, Chu XJ, Crespo A, Dwyer MP, Keertikar K, Morriello GJ, Stamford AW, Waddell ST, Zhong B, Hu B, Ji T, Diamond TL, Bahnck-Teets C, Carroll SS, Fay JF, Min X, Morris W, Ballard JE, Miller MD, McCauley JA. Bungard CJ, et al. Among authors: morriello gj. ACS Med Chem Lett. 2017 Nov 13;8(12):1292-1297. doi: 10.1021/acsmedchemlett.7b00386. eCollection 2017 Dec 14. ACS Med Chem Lett. 2017. PMID: 29259750 Free PMC article.
Structure-Guided Discovery of Aminoquinazolines as Brain-Penetrant and Selective LRRK2 Inhibitors.
Keylor MH, Gulati A, Kattar SD, Johnson RE, Chau RW, Margrey KA, Ardolino MJ, Zarate C, Poremba KE, Simov V, Morriello GJ, Acton JJ, Pio B, Yan X, Palte RL, McMinn SE, Nogle L, Lesburg CA, Adpressa D, Lin S, Neelamkavil S, Liu P, Su J, Hegde LG, Woodhouse JD, Faltus R, Xiong T, Ciaccio PJ, Piesvaux J, Otte KM, Wood HB, Kennedy ME, Bennett DJ, DiMauro EF, Fell MJ, Fuller PH. Keylor MH, et al. Among authors: morriello gj. J Med Chem. 2022 Jan 13;65(1):838-856. doi: 10.1021/acs.jmedchem.1c01968. Epub 2021 Dec 30. J Med Chem. 2022. PMID: 34967623
Discovery and Optimization of N-Heteroaryl Indazole LRRK2 Inhibitors.
Logan KM, Kaplan W, Simov V, Zhou H, Li D, Torres L, Morriello GJ, Acton JJ, Pio B, Chen YH, Keylor MH, Johnson R, Kattar SD, Chau R, Yan X, Ardolino M, Zarate C, Otte KM, Palte RL, Xiong T, McMinn SE, Lin S, Neelamkavil SF, Liu P, Su J, Hegde LG, Woodhouse JD, Moy LY, Ciaccio PJ, Piesvaux J, Zebisch M, Henry C, Barker J, Wood HB, Kennedy ME, DiMauro EF, Fell MJ, Fuller PH. Logan KM, et al. Among authors: morriello gj. J Med Chem. 2024 Sep 26;67(18):16807-16819. doi: 10.1021/acs.jmedchem.4c01627. Epub 2024 Sep 4. J Med Chem. 2024. PMID: 39231262
1-[2(R)-(2-amino-2-methylpropionylamino)-3-(1H-indol-3-yl)propionyl]- 3-benzylpiperidine-3(S)-carboxylic acid ethyl ester (L-163,540): a potent, orally bioavailable, and short-duration growth hormone secretagogue.
Yang L, Morriello G, Patchett AA, Leung K, Jacks T, Cheng K, Schleim KD, Feeney W, Chan WW, Chiu SH, Smith RG. Yang L, et al. J Med Chem. 1998 Jul 2;41(14):2439-41. doi: 10.1021/jm9800191. J Med Chem. 1998. PMID: 9651148 No abstract available.
Fused bicyclic pyrrolizinones as new scaffolds for human NK1 antagonists.
Morriello GJ, Devita RJ, Mills SG, Young JR, Lin P, Doss G, Chicchi GG, Demartino J, Kurtz MM, Tsao KL, Carlson E, Townson K, Wheeldon A, Boyce S, Collinson N, Rupniak N, Moore S. Morriello GJ, et al. Bioorg Med Chem. 2008 Mar 1;16(5):2156-70. doi: 10.1016/j.bmc.2007.11.081. Epub 2007 Dec 5. Bioorg Med Chem. 2008. PMID: 18248994
25 results