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Page 1
Trisubstituted thiazoles as potent and selective inhibitors of Plasmodium falciparum protein kinase G (PfPKG).
Tsagris DJ, Birchall K, Bouloc N, Large JM, Merritt A, Smiljanic-Hurley E, Wheldon M, Ansell KH, Kettleborough C, Whalley D, Stewart LB, Bowyer PW, Baker DA, Osborne SA. Tsagris DJ, et al. Among authors: wheldon m. Bioorg Med Chem Lett. 2018 Oct 15;28(19):3168-3173. doi: 10.1016/j.bmcl.2018.08.028. Epub 2018 Aug 27. Bioorg Med Chem Lett. 2018. PMID: 30174152 Free PMC article.
A potent series targeting the malarial cGMP-dependent protein kinase clears infection and blocks transmission.
Baker DA, Stewart LB, Large JM, Bowyer PW, Ansell KH, Jiménez-Díaz MB, El Bakkouri M, Birchall K, Dechering KJ, Bouloc NS, Coombs PJ, Whalley D, Harding DJ, Smiljanic-Hurley E, Wheldon MC, Walker EM, Dessens JT, Lafuente MJ, Sanz LM, Gamo FJ, Ferrer SB, Hui R, Bousema T, Angulo-Barturén I, Merritt AT, Croft SL, Gutteridge WE, Kettleborough CA, Osborne SA. Baker DA, et al. Among authors: wheldon mc. Nat Commun. 2017 Sep 5;8(1):430. doi: 10.1038/s41467-017-00572-x. Nat Commun. 2017. PMID: 28874661 Free PMC article.
Potent inhibitors of malarial P. Falciparum protein kinase G: Improving the cell activity of a series of imidazopyridines.
Large JM, Birchall K, Bouloc NS, Merritt AT, Smiljanic-Hurley E, Tsagris DJ, Wheldon MC, Ansell KH, Coombs PJ, Kettleborough CA, Whalley D, Stewart LB, Bowyer PW, Baker DA, Osborne SA. Large JM, et al. Among authors: wheldon mc. Bioorg Med Chem Lett. 2019 Feb 1;29(3):509-514. doi: 10.1016/j.bmcl.2018.11.039. Epub 2018 Nov 20. Bioorg Med Chem Lett. 2019. PMID: 30553738 Free PMC article.
Potent bicyclic inhibitors of malarial cGMP-dependent protein kinase: approaches to combining improvements in cell potency, selectivity and structural novelty.
Large JM, Birchall K, Bouloc NS, Merritt AT, Smiljanic-Hurley E, Tsagris DJ, Wheldon MC, Ansell KH, Coombs PJ, Kettleborough CA, Whalley D, Stewart LB, Bowyer PW, Baker DA, Osborne SA. Large JM, et al. Among authors: wheldon mc. Bioorg Med Chem Lett. 2019 Oct 1;29(19):126610. doi: 10.1016/j.bmcl.2019.08.014. Epub 2019 Aug 9. Bioorg Med Chem Lett. 2019. PMID: 31471167 Free PMC article.
Design and Synthesis of 56 Shape-Diverse 3D Fragments.
Downes TD, Jones SP, Klein HF, Wheldon MC, Atobe M, Bond PS, Firth JD, Chan NS, Waddelove L, Hubbard RE, Blakemore DC, De Fusco C, Roughley SD, Vidler LR, Whatton MA, Woolford AJ, Wrigley GL, O'Brien P. Downes TD, et al. Among authors: wheldon mc. Chemistry. 2020 Jul 22;26(41):8969-8975. doi: 10.1002/chem.202001123. Epub 2020 Jul 8. Chemistry. 2020. PMID: 32315100 Free PMC article.
Exploration of piperidine 3D fragment chemical space: synthesis and 3D shape analysis of fragments derived from 20 regio- and diastereoisomers of methyl substituted pipecolinates.
Jones SP, Firth JD, Wheldon MC, Atobe M, Hubbard RE, Blakemore DC, De Fusco C, Lucas SCC, Roughley SD, Vidler LR, Whatton MA, Woolford AJ, Wrigley GL, O'Brien P. Jones SP, et al. Among authors: wheldon mc. RSC Med Chem. 2022 Oct 11;13(12):1614-1620. doi: 10.1039/d2md00239f. eCollection 2022 Dec 14. RSC Med Chem. 2022. PMID: 36545433 Free PMC article.
18 results