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Discovery of Potent and Orally Bioavailable Pyridine N-Oxide-Based Factor XIa Inhibitors through Exploiting Nonclassical Interactions.
Xu G, Liu Z, Wang X, Lu T, DesJarlais RL, Thieu T, Zhang J, Devine ZH, Du F, Li Q, Milligan CM, Shaffer P, Cedervall PE, Spurlino JC, Stratton CF, Pietrak B, Szewczuk LM, Wong V, Steele RA, Bruinzeel W, Chintala M, Silva J, Gaul MD, Macielag MJ, Nargund R. Xu G, et al. Among authors: silva j. J Med Chem. 2022 Aug 11;65(15):10419-10440. doi: 10.1021/acs.jmedchem.2c00442. Epub 2022 Jul 21. J Med Chem. 2022. PMID: 35862732
Discovery of novel benzo[b]thiophene tetrazoles as non-carboxylate GPR40 agonists.
Huang H, Winters MP, Meegalla SK, Arnoult E, Paul Lee S, Zhao S, Martin T, Rady B, Liu J, Towers M, Otieno M, Xu F, Lim HK, Silva J, Pocai A, Player MR. Huang H, et al. Among authors: silva j. Bioorg Med Chem Lett. 2018 Feb 1;28(3):429-436. doi: 10.1016/j.bmcl.2017.12.022. Epub 2017 Dec 12. Bioorg Med Chem Lett. 2018. PMID: 29258772
Discovery of a novel potent GPR40 full agonist.
Meegalla SK, Huang H, Martin T, Xu J, Zhao S, Liu J, Hall M, Gunnet J, Wang Y, Rady B, Silva J, Otieno M, Arnoult E, Paul Lee S, Pocai A, Player MR. Meegalla SK, et al. Among authors: silva j. Bioorg Med Chem Lett. 2018 Feb 15;28(4):720-726. doi: 10.1016/j.bmcl.2018.01.013. Epub 2018 Jan 12. Bioorg Med Chem Lett. 2018. PMID: 29366647
Design, synthesis and biological evaluation of (2S,3R,4R,5S,6R)-5-fluoro-6-(hydroxymethyl)-2-aryltetrahydro-2H-pyran-3,4-diols as potent and orally active SGLT dual inhibitors.
Xu G, Gaul MD, Kuo GH, Du F, Xu JZ, Wallace N, Hinke S, Kirchner T, Silva J, Huebert ND, Lee S, Murray W, Liang Y, Demarest K. Xu G, et al. Among authors: silva j. Bioorg Med Chem Lett. 2018 Nov 15;28(21):3446-3453. doi: 10.1016/j.bmcl.2018.09.025. Epub 2018 Sep 19. Bioorg Med Chem Lett. 2018. PMID: 30268701
Discovery of a GPR40 Superagonist: The Impact of Aryl Propionic Acid α-Fluorination.
Huang H, Meegalla SK, Lanter JC, Winters MP, Zhao S, Littrell J, Qi J, Rady B, Lee PS, Liu J, Martin T, Lam WW, Xu F, Lim HK, Wilde T, Silva J, Otieno M, Pocai A, Player MR. Huang H, et al. Among authors: silva j. ACS Med Chem Lett. 2018 Dec 3;10(1):16-21. doi: 10.1021/acsmedchemlett.8b00444. eCollection 2019 Jan 10. ACS Med Chem Lett. 2018. PMID: 30655940 Free PMC article.
Metabolism and disposition of JNJ-10450232 (NTM-006) in rats, dogs, monkeys and humans.
Lim HK, Chen J, Lam W, Gong Y, Leclercq L, Silva J, Salter R, Berwaerts J, Gelotte CK, Vakil AM, Eichenbaum GE, Kuffner EK, Flores CM. Lim HK, et al. Among authors: silva j. Regul Toxicol Pharmacol. 2023 Mar 16:105379. doi: 10.1016/j.yrtph.2023.105379. Online ahead of print. Regul Toxicol Pharmacol. 2023. PMID: 36931586 Free article.
Metabolism and excretion of canagliflozin in mice, rats, dogs, and humans.
Mamidi RN, Cuyckens F, Chen J, Scheers E, Kalamaridis D, Lin R, Silva J, Sha S, Evans DC, Kelley MF, Devineni D, Johnson MD, Lim HK. Mamidi RN, et al. Among authors: silva j. Drug Metab Dispos. 2014 May;42(5):903-16. doi: 10.1124/dmd.113.056440. Epub 2014 Feb 25. Drug Metab Dispos. 2014. PMID: 24568888 Clinical Trial.
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