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1,3,8-Triazaspiro[4.5]decane-2,4-diones as efficacious pan-inhibitors of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) for the treatment of anemia.
Vachal P, Miao S, Pierce JM, Guiadeen D, Colandrea VJ, Wyvratt MJ, Salowe SP, Sonatore LM, Milligan JA, Hajdu R, Gollapudi A, Keohane CA, Lingham RB, Mandala SM, DeMartino JA, Tong X, Wolff M, Steinhuebel D, Kieczykowski GR, Fleitz FJ, Chapman K, Athanasopoulos J, Adam G, Akyuz CD, Jena DK, Lusen JW, Meng J, Stein BD, Xia L, Sherer EC, Hale JJ. Vachal P, et al. J Med Chem. 2012 Apr 12;55(7):2945-59. doi: 10.1021/jm201542d. Epub 2012 Feb 27. J Med Chem. 2012. PMID: 22364528
Effects of anacetrapib on plasma lipids, apolipoproteins and PCSK9 in healthy, lean rhesus macaques.
Roddy TP, McLaren DG, Chen Y, Xie D, Dunn K, Kulick A, Szeto D, Forrest G, Albanese K, Donnelly M, Gai C, Gewain A, Lederman H, Jensen KK, Ai X, Vachal P, Akinsanya KO, Cleary MA, Previs SF, Dansky HM, Johns DG. Roddy TP, et al. Among authors: vachal p. Eur J Pharmacol. 2014 Oct 5;740:410-6. doi: 10.1016/j.ejphar.2014.04.015. Epub 2014 Apr 21. Eur J Pharmacol. 2014. PMID: 24769414
Discovery of Novel Indoline Cholesterol Ester Transfer Protein Inhibitors (CETP) through a Structure-Guided Approach.
Wilson JE, Kurukulasuriya R, Reibarkh M, Reiter M, Zwicker A, Zhao K, Zhang F, Anand R, Colandrea VJ, Cumiskey AM, Crespo A, Duffy RA, Murphy BA, Mitra K, Johns DG, Duffy JL, Vachal P. Wilson JE, et al. Among authors: vachal p. ACS Med Chem Lett. 2016 Jan 4;7(3):261-5. doi: 10.1021/acsmedchemlett.5b00404. eCollection 2016 Mar 10. ACS Med Chem Lett. 2016. PMID: 26985312 Free PMC article.
Microscale High-Throughput Experimentation as an Enabling Technology in Drug Discovery: Application in the Discovery of (Piperidinyl)pyridinyl-1H-benzimidazole Diacylglycerol Acyltransferase 1 Inhibitors.
Cernak T, Gesmundo NJ, Dykstra K, Yu Y, Wu Z, Shi ZC, Vachal P, Sperbeck D, He S, Murphy BA, Sonatore L, Williams S, Madeira M, Verras A, Reiter M, Lee CH, Cuff J, Sherer EC, Kuethe J, Goble S, Perrotto N, Pinto S, Shen DM, Nargund R, Balkovec J, DeVita RJ, Dreher SD. Cernak T, et al. Among authors: vachal p. J Med Chem. 2017 May 11;60(9):3594-3605. doi: 10.1021/acs.jmedchem.6b01543. Epub 2017 Mar 2. J Med Chem. 2017. PMID: 28252959
Accelerating the discovery of DGAT1 inhibitors through the application of parallel medicinal chemistry (PMC).
Yu Y, Wu Z, Shi ZC, He S, Lai Z, Cernak TA, Vachal P, Liu M, Liu J, Hong Q, Jian T, Guiadeen D, Krikorian A, Sperbeck DM, Verras A, Sonatore LM, Murphy BA, Wiltsie J, Chung CC, Gorski JN, Liu J, Xiao J, Wolff M, Tong SX, Madeira M, Karanam BV, Shen DM, Balkovec JM, De Vita RJ, Pinto S, Nargund RP. Yu Y, et al. Among authors: vachal p. Bioorg Med Chem Lett. 2019 Jun 1;29(11):1380-1385. doi: 10.1016/j.bmcl.2019.03.039. Epub 2019 Mar 27. Bioorg Med Chem Lett. 2019. PMID: 30952592
Development of indazole mineralocorticoid receptor antagonists and investigation into their selective late-stage functionalization.
Liu K, Kurukulasuriya R, Dykstra K, DiMichelle L, Liu J, Vachal P, Ogawa A, DeVita RJ, Shen DM, Tan Q, Chen Y, Gauthier D, Verras A, Crespo A, Zamlynny B, Madwed J, Hoek M, Bateman T, Yang YF, Houk KN, Krska S, Cernak T. Liu K, et al. Among authors: vachal p. Bioorg Med Chem Lett. 2019 Jul 15;29(14):1854-1858. doi: 10.1016/j.bmcl.2019.04.024. Epub 2019 Apr 15. Bioorg Med Chem Lett. 2019. PMID: 31104995
Synthesis of HDAC Inhibitor Libraries via Microscale Workflow.
Dykstra KD, Streckfuss E, Liu M, Liu J, Yu Y, Wang M, Kozlowski JA, Myers RW, Buevich AV, Maletic MM, Vachal P, Krska SW. Dykstra KD, et al. Among authors: vachal p. ACS Med Chem Lett. 2021 Feb 8;12(3):337-342. doi: 10.1021/acsmedchemlett.0c00596. eCollection 2021 Mar 11. ACS Med Chem Lett. 2021. PMID: 33738059 Free PMC article.
28 results