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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: whalley d. 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.
Biochemical and antiparasitic properties of inhibitors of the Plasmodium falciparum calcium-dependent protein kinase PfCDPK1.
Ansell KH, Jones HM, Whalley D, Hearn A, Taylor DL, Patin EC, Chapman TM, Osborne SA, Wallace C, Birchall K, Large J, Bouloc N, Smiljanic-Hurley E, Clough B, Moon RW, Green JL, Holder AA. Ansell KH, et al. Among authors: whalley d. Antimicrob Agents Chemother. 2014 Oct;58(10):6032-43. doi: 10.1128/AAC.02959-14. Epub 2014 Jul 28. Antimicrob Agents Chemother. 2014. PMID: 25070106 Free PMC article.
Imidazopyridazine Inhibitors of Plasmodium falciparum Calcium-Dependent Protein Kinase 1 Also Target Cyclic GMP-Dependent Protein Kinase and Heat Shock Protein 90 To Kill the Parasite at Different Stages of Intracellular Development.
Green JL, Moon RW, Whalley D, Bowyer PW, Wallace C, Rochani A, Nageshan RK, Howell SA, Grainger M, Jones HM, Ansell KH, Chapman TM, Taylor DL, Osborne SA, Baker DA, Tatu U, Holder AA. Green JL, et al. Among authors: whalley d. Antimicrob Agents Chemother. 2015 Dec 28;60(3):1464-75. doi: 10.1128/AAC.01748-15. Antimicrob Agents Chemother. 2015. PMID: 26711771 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: whalley d. 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: whalley d. 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: whalley d. 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.
Effective inhibitors of the essential kinase PknB and their potential as anti-mycobacterial agents.
Lougheed KE, Osborne SA, Saxty B, Whalley D, Chapman T, Bouloc N, Chugh J, Nott TJ, Patel D, Spivey VL, Kettleborough CA, Bryans JS, Taylor DL, Smerdon SJ, Buxton RS. Lougheed KE, et al. Among authors: whalley d. Tuberculosis (Edinb). 2011 Jul;91(4):277-86. doi: 10.1016/j.tube.2011.03.005. Epub 2011 Apr 11. Tuberculosis (Edinb). 2011. PMID: 21482481 Free PMC article.
194 results