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Imitation of β-lactam binding enables broad-spectrum metallo-β-lactamase inhibitors.
Nat Chem. 2022 Jan;14(1):15-24. doi: 10.1038/s41557-021-00831-x. Epub 2021 Dec 13.
Nat Chem. 2022.
PMID: 34903857
Pan-NS3 protease inhibitors of hepatitis C virus based on an R3-elongated pyrazinone scaffold.
Belfrage AK, Abdurakhmanov E, Åkerblom E, Brandt P, Alogheli H, Neyts J, Danielson UH, Sandström A.
Belfrage AK, et al.
Eur J Med Chem. 2018 Mar 25;148:453-464. doi: 10.1016/j.ejmech.2018.02.032. Epub 2018 Feb 13.
Eur J Med Chem. 2018.
PMID: 29477077
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Discovery of pyrazinone based compounds that potently inhibit the drug-resistant enzyme variant R155K of the hepatitis C virus NS3 protease.
Belfrage AK, Abdurakhmanov E, Kerblom E, Brandt P, Oshalim A, Gising J, Skogh A, Neyts J, Danielson UH, Sandström A.
Belfrage AK, et al.
Bioorg Med Chem. 2016 Jun 15;24(12):2603-20. doi: 10.1016/j.bmc.2016.03.066. Epub 2016 Apr 8.
Bioorg Med Chem. 2016.
PMID: 27160057
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ENABLE: an engine for European antibacterial drug discovery and development.
Olliver M, Griestop L, Hughes D, Belfrage AK, Gising J, Baranczewski P, Vingsbo Lundberg C, Karlén A.
Olliver M, et al. Among authors: belfrage ak.
Nat Rev Drug Discov. 2021 Jun;20(6):407-408. doi: 10.1038/d41573-021-00074-y.
Nat Rev Drug Discov. 2021.
PMID: 33948003
No abstract available.
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Achiral pyrazinone-based inhibitors of the hepatitis C virus NS3 protease and drug-resistant variants with elongated substituents directed toward the S2 pocket.
Gising J, Belfrage AK, Alogheli H, Ehrenberg A, Åkerblom E, Svensson R, Artursson P, Karlén A, Danielson UH, Larhed M, Sandström A.
Gising J, et al. Among authors: belfrage ak.
J Med Chem. 2014 Mar 13;57(5):1790-801. doi: 10.1021/jm301887f. Epub 2013 Apr 2.
J Med Chem. 2014.
PMID: 23517538
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Design and synthesis of potent inhibitors of the malaria aspartyl proteases plasmepsin I and II. Use of solid-phase synthesis to explore novel statine motifs.
Johansson PO, Chen Y, Belfrage AK, Blackman MJ, Kvarnström I, Jansson K, Vrang L, Hamelink E, Hallberg A, Rosenquist A, Samuelsson B.
Johansson PO, et al. Among authors: belfrage ak.
J Med Chem. 2004 Jun 17;47(13):3353-66. doi: 10.1021/jm031106i.
J Med Chem. 2004.
PMID: 15189032
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Synthesis and SAR of potent inhibitors of the Hepatitis C virus NS3/4A protease: exploration of P2 quinazoline substituents.
Nilsson M, Belfrage AK, Lindström S, Wähling H, Lindquist C, Ayesa S, Kahnberg P, Pelcman M, Benkestock K, Agback T, Vrang L, Terelius Y, Wikström K, Hamelink E, Rydergård C, Edlund M, Eneroth A, Raboisson P, Lin TI, de Kock H, Wigerinck P, Simmen K, Samuelsson B, Rosenquist S.
Nilsson M, et al. Among authors: belfrage ak.
Bioorg Med Chem Lett. 2010 Jul 15;20(14):4004-11. doi: 10.1016/j.bmcl.2010.05.029. Epub 2010 May 21.
Bioorg Med Chem Lett. 2010.
PMID: 20541405
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Discovery of 4'-azido-2'-deoxy-2'-C-methyl cytidine and prodrugs thereof: a potent inhibitor of Hepatitis C virus replication.
Nilsson M, Kalayanov G, Winqvist A, Pinho P, Sund C, Zhou XX, Wähling H, Belfrage AK, Pelcman M, Agback T, Benckestock K, Wikström K, Boothee M, Lindqvist A, Rydegård C, Jonckers TH, Vandyck K, Raboisson P, Lin TI, Lachau-Durand S, de Kock H, Smith DB, Martin JA, Klumpp K, Simmen K, Vrang L, Terelius Y, Samuelsson B, Rosenquist S, Johansson NG.
Nilsson M, et al. Among authors: belfrage ak.
Bioorg Med Chem Lett. 2012 May 1;22(9):3265-8. doi: 10.1016/j.bmcl.2012.03.021. Epub 2012 Mar 16.
Bioorg Med Chem Lett. 2012.
PMID: 22472694
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