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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: neelamkavil s. 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 MK-8831, A Novel Spiro-Proline Macrocycle as a Pan-Genotypic HCV-NS3/4a Protease Inhibitor.
Neelamkavil SF, Agrawal S, Bara T, Bennett C, Bhat S, Biswas D, Brockunier L, Buist N, Burnette D, Cartwright M, Chackalamannil S, Chase R, Chelliah M, Chen A, Clasby M, Colandrea VJ, Davies IW, Eagen K, Guo Z, Han Y, Howe J, Jayne C, Josien H, Kargman S, Marcantonio K, Miao S, Miller R, Nolting A, Pinto P, Rajagopalan M, Ruck RT, Shah U, Soriano A, Sperbeck D, Velazquez F, Wu J, Xia Y, Venkatraman S. Neelamkavil SF, et al. ACS Med Chem Lett. 2015 Dec 22;7(1):111-6. doi: 10.1021/acsmedchemlett.5b00425. eCollection 2016 Jan 14. ACS Med Chem Lett. 2015. PMID: 26819676 Free PMC article.
Design and Synthesis of P2-P4 Macrocycles Containing a Unique Spirocyclic Proline: A New Class of HCV NS3/4A Inhibitors.
Velázquez F, Chelliah M, Clasby M, Guo Z, Howe J, Miller R, Neelamkavil S, Shah U, Soriano A, Xia Y, Venkatraman S, Chackalamannil S, Davies IW. Velázquez F, et al. Among authors: neelamkavil s. ACS Med Chem Lett. 2016 Oct 17;7(12):1173-1178. doi: 10.1021/acsmedchemlett.6b00321. eCollection 2016 Dec 8. ACS Med Chem Lett. 2016. PMID: 27994759 Free PMC article.
Discovery of MK-8282 as a Potent G-Protein-Coupled Receptor 119 Agonist for the Treatment of Type 2 Diabetes.
Neelamkavil SF, Stamford AW, Kowalski T, Biswas D, Boyle C, Chackalamannil S, Xia Y, Jayne C, Neustadt B, Hao J, Liu H, Dai X, Baker H, Hawes B, O'Neill K, Tang H, Greenlee WJ. Neelamkavil SF, et al. ACS Med Chem Lett. 2018 Apr 10;9(5):457-461. doi: 10.1021/acsmedchemlett.8b00073. eCollection 2018 May 10. ACS Med Chem Lett. 2018. PMID: 29795759 Free PMC article.
Design and synthesis of novel proline based factor XIa selective inhibitors as leads for potential new anticoagulants.
Hussain Z, Cooke AJ, Neelamkavil S, Brown L, Carswell E, Geissler WM, Guo Z, Hawes B, Kelly TM, Kiyoi Y, Lai K, Lesburg C, Pow E, Zang Y, Wood HB, Edmondson SD, Liu W. Hussain Z, et al. Among authors: neelamkavil s. Bioorg Med Chem Lett. 2020 Aug 15;30(16):127072. doi: 10.1016/j.bmcl.2020.127072. Epub 2020 Feb 29. Bioorg Med Chem Lett. 2020. PMID: 32340773
Discovery of hydroxy pyrimidine Factor IXa inhibitors.
Jayne CL, Andreani T, Chan TY, Chelliah MV, Clasby MC, Dwyer M, Eagen KA, Fried S, Greenlee WJ, Guo Z, Hawes B, Hruza A, Ingram R, Keertikar KM, Neelamkavil S, Reichert P, Xia Y, Chackalamannil S. Jayne CL, et al. Among authors: neelamkavil s. Bioorg Med Chem Lett. 2020 Aug 1;30(15):127279. doi: 10.1016/j.bmcl.2020.127279. Epub 2020 May 23. Bioorg Med Chem Lett. 2020. PMID: 32527459
Optimization of brain-penetrant picolinamide derived leucine-rich repeat kinase 2 (LRRK2) inhibitors.
Gulati A, Yeung CS, Lapointe B, Kattar SD, Gunaydin H, Scott JD, Childers KK, Methot JL, Simov V, Kurukulasuriya R, Pio B, Morriello GJ, Liu P, Tang H, Neelamkavil S, Wood HB, Rada VL, Ardolino MJ, Yan XC, Palte R, Otte K, Faltus R, Woodhouse J, Hegde LG, Ciaccio P, Minnihan EC, DiMauro EF, Fell MJ, Fuller PH, Ellis JM. Gulati A, et al. Among authors: neelamkavil s. RSC Med Chem. 2021 Jun 4;12(7):1164-1173. doi: 10.1039/d1md00097g. eCollection 2021 Jul 21. RSC Med Chem. 2021. PMID: 34355182 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: neelamkavil s. 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: neelamkavil sf. 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
18 results