Robert Owen Hughes

Affiliations: 
2002 Scripps Research Institute, La Jolla, La Jolla, CA, United States 
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K. C. Nicolaou grad student 2002 Scripps Institute
 (Strategies for the rapid discovery of antibacterial agents: Studies on vancomycin and psammaplin A.)
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Schnute ME, Benoit SE, Buchler IP, et al. (2019) Aminopyrazole Carboxamide Bruton's Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning. Acs Medicinal Chemistry Letters. 10: 80-85
Li X, Anderson M, Collin D, et al. (2017) Structural studies unravel the active conformation of apo RORγt nuclear receptor and a common inverse agonism of two diverse classes of RORγt inhibitors. The Journal of Biological Chemistry
Xue CB, Wang A, Han Q, et al. (2011) Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist. Acs Medicinal Chemistry Letters. 2: 913-8
Hughes RO, Maddux T, Joseph Rogier D, et al. (2011) Investigation of the pyrazinones as PDE5 inhibitors: evaluation of regioisomeric projections into the solvent region. Bioorganic & Medicinal Chemistry Letters. 21: 6348-52
Trujillo JI, Huang W, Hughes RO, et al. (2011) Design and synthesis of novel CCR2 antagonists: investigation of non-aryl/heteroaryl binding motifs. Bioorganic & Medicinal Chemistry Letters. 21: 1827-31
Zheng C, Cao G, Xia M, et al. (2011) Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist. Bioorganic & Medicinal Chemistry Letters. 21: 1442-6
Tollefson MB, Acker BA, Jacobsen EJ, et al. (2010) 1-(2-Ethoxyethyl)-1H-pyrazolo[4,3-d]pyrimidines as potent phosphodiesterase 5 (PDE5) inhibitors. Bioorganic & Medicinal Chemistry Letters. 20: 3120-4
Tollefson MB, Acker BA, Jacobsen EJ, et al. (2010) 1-(2-(2,2,2-trifluoroethoxy)ethyl-1H-pyrazolo[4,3-d]pyrimidines as potent phosphodiesterase 5 (PDE5) inhibitors. Bioorganic & Medicinal Chemistry Letters. 20: 3125-8
Hughes RO, Rogier DJ, Jacobsen EJ, et al. (2010) Design, synthesis, and biological evaluation of 3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one, a potent, orally active, brain penetrant inhibitor of phosphodiesterase 5 (PDE5). Journal of Medicinal Chemistry. 53: 2656-60
Hughes RO, Walker JK, Joseph Rogier D, et al. (2009) Optimization of the aminopyridopyrazinones class of PDE5 inhibitors: Discovery of 3-[(trans-4-hydroxycyclohexyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one Bioorganic and Medicinal Chemistry Letters. 19: 5209-5213
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