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Page 1
Escaping from Flatland: Antimalarial Activity of sp3-Rich Bridged Pyrrolidine Derivatives.
Cox B, Duffy J, Zdorichenko V, Bellanger C, Hurcum J, Laleu B, Booker-Milburn KI, Elliott LD, Robertson-Ralph M, Swain CJ, Bishop SJ, Hallyburton I, Anderson M. Cox B, et al. Among authors: duffy j. ACS Med Chem Lett. 2020 Nov 10;11(12):2497-2503. doi: 10.1021/acsmedchemlett.0c00486. eCollection 2020 Dec 10. ACS Med Chem Lett. 2020. PMID: 33335673 Free PMC article.
Identification of Fast-Acting 2,6-Disubstituted Imidazopyridines That Are Efficacious in the in Vivo Humanized Plasmodium falciparum NODscidIL2Rγ null Mouse Model of Malaria.
Nchinda AT, Le Manach C, Paquet T, Gonzàlez Cabrera D, Wicht KJ, Brunschwig C, Njoroge M, Abay E, Taylor D, Lawrence N, Wittlin S, Jiménez-Díaz MB, Santos Martínez M, Ferrer S, Angulo-Barturen I, Lafuente-Monasterio MJ, Duffy J, Burrows J, Street LJ, Chibale K. Nchinda AT, et al. Among authors: duffy j. J Med Chem. 2018 May 10;61(9):4213-4227. doi: 10.1021/acs.jmedchem.8b00382. Epub 2018 Apr 27. J Med Chem. 2018. PMID: 29665687
Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis.
Baragaña B, Forte B, Choi R, Nakazawa Hewitt S, Bueren-Calabuig JA, Pisco JP, Peet C, Dranow DM, Robinson DA, Jansen C, Norcross NR, Vinayak S, Anderson M, Brooks CF, Cooper CA, Damerow S, Delves M, Dowers K, Duffy J, Edwards TE, Hallyburton I, Horst BG, Hulverson MA, Ferguson L, Jiménez-Díaz MB, Jumani RS, Lorimer DD, Love MS, Maher S, Matthews H, McNamara CW, Miller P, O'Neill S, Ojo KK, Osuna-Cabello M, Pinto E, Post J, Riley J, Rottmann M, Sanz LM, Scullion P, Sharma A, Shepherd SM, Shishikura Y, Simeons FRC, Stebbins EE, Stojanovski L, Straschil U, Tamaki FK, Tamjar J, Torrie LS, Vantaux A, Witkowski B, Wittlin S, Yogavel M, Zuccotto F, Angulo-Barturen I, Sinden R, Baum J, Gamo FJ, Mäser P, Kyle DE, Winzeler EA, Myler PJ, Wyatt PG, Floyd D, Matthews D, Sharma A, Striepen B, Huston CD, Gray DW, Fairlamb AH, Pisliakov AV, Walpole C, Read KD, Van Voorhis WC, Gilbert IH. Baragaña B, et al. Among authors: duffy j. Proc Natl Acad Sci U S A. 2019 Apr 2;116(14):7015-7020. doi: 10.1073/pnas.1814685116. Epub 2019 Mar 20. Proc Natl Acad Sci U S A. 2019. PMID: 30894487 Free PMC article.
Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and In Vivo Efficacy in the Plasmodium falciparum NSG Mouse Model.
Horatscheck A, Andrijevic A, Nchinda AT, Le Manach C, Paquet T, Khonde LP, Dam J, Pawar K, Taylor D, Lawrence N, Brunschwig C, Gibhard L, Njoroge M, Reader J, van der Watt M, Wicht K, de Sousa ACC, Okombo J, Maepa K, Egan TJ, Birkholtz LM, Basarab GS, Wittlin S, Fish PV, Street LJ, Duffy J, Chibale K. Horatscheck A, et al. Among authors: duffy j. J Med Chem. 2020 Nov 12;63(21):13013-13030. doi: 10.1021/acs.jmedchem.0c01411. Epub 2020 Oct 25. J Med Chem. 2020. PMID: 33103428 Free PMC article.
Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite Plasmodium falciparum and Optimization Efforts.
Le Manach C, Dam J, Woodland JG, Kaur G, Khonde LP, Brunschwig C, Njoroge M, Wicht KJ, Horatscheck A, Paquet T, Boyle GA, Gibhard L, Taylor D, Lawrence N, Yeo T, Mok S, Eastman RT, Dorjsuren D, Talley DC, Guo H, Simeonov A, Reader J, van der Watt M, Erlank E, Venter N, Zawada JW, Aswat A, Nardini L, Coetzer TL, Lauterbach SB, Bezuidenhout BC, Theron A, Mancama D, Koekemoer LL, Birkholtz LM, Wittlin S, Delves M, Ottilie S, Winzeler EA, von Geldern TW, Smith D, Fidock DA, Street LJ, Basarab GS, Duffy J, Chibale K. Le Manach C, et al. Among authors: duffy j. J Med Chem. 2021 Feb 25;64(4):2291-2309. doi: 10.1021/acs.jmedchem.1c00034. Epub 2021 Feb 12. J Med Chem. 2021. PMID: 33573376
Replenishing the malaria drug discovery pipeline: Screening and hit evaluation of the MMV Hit Generation Library 1 (HGL1) against asexual blood stage Plasmodium falciparum, using a nano luciferase reporter read-out.
Dechering KJ, Timmerman M, Rensen K, Koolen KMJ, Honarnejad S, Vos MW, Huijs T, Henderson RWM, Chenu E, Laleu B, Montefiore BC, Segall MD, Mills JEJ, Guantai EM, Duffy J, Duffey M. Dechering KJ, et al. Among authors: duffy j. SLAS Discov. 2022 Sep;27(6):337-348. doi: 10.1016/j.slasd.2022.07.002. Epub 2022 Jul 21. SLAS Discov. 2022. PMID: 35872229 Free article.
Exploring a Tetrahydroquinoline Antimalarial Hit from the Medicines for Malaria Pathogen Box and Identification of its Mode of Resistance as PfeEF2.
Laleu B, Rubiano K, Yeo T, Hallyburton I, Anderson M, Crespo-Fernandez B, Gamo FJ, Antonova-Koch Y, Orjuela-Sanchez P, Wittlin S, Jana GP, Maity BC, Chenu E, Duffy J, Sjö P, Waterson D, Winzeler E, Guantai E, Fidock DA, Hansson TG. Laleu B, et al. Among authors: duffy j. ChemMedChem. 2022 Nov 18;17(22):e202200393. doi: 10.1002/cmdc.202200393. Epub 2022 Oct 13. ChemMedChem. 2022. PMID: 36129427 Free PMC article.
Preliminary Structure-Activity Relationship Study of the MMV Pathogen Box Compound MMV675968 (2,4-Diaminoquinazoline) Unveils Novel Inhibitors of Trypanosoma brucei brucei.
Dize D, Tata RB, Keumoe R, Kouipou Toghueo RM, Tchatat MB, Njanpa CN, Tchuenguia VC, Yamthe LT, Fokou PVT, Laleu B, Duffy J, Bishop OT, Boyom FF. Dize D, et al. Among authors: duffy j. Molecules. 2022 Oct 4;27(19):6574. doi: 10.3390/molecules27196574. Molecules. 2022. PMID: 36235118 Free PMC article.
Antimalarial Lead-Optimization Studies on a 2,6-Imidazopyridine Series within a Constrained Chemical Space To Circumvent Atypical Dose-Response Curves against Multidrug Resistant Parasite Strains.
Le Manach C, Paquet T, Wicht K, Nchinda AT, Brunschwig C, Njoroge M, Gibhard L, Taylor D, Lawrence N, Wittlin S, Eyermann CJ, Basarab GS, Duffy J, Fish PV, Street LJ, Chibale K. Le Manach C, et al. Among authors: duffy j. J Med Chem. 2018 Oct 25;61(20):9371-9385. doi: 10.1021/acs.jmedchem.8b01333. Epub 2018 Oct 16. J Med Chem. 2018. PMID: 30256636
Generation of a mutator parasite to drive resistome discovery in Plasmodium falciparum.
Kümpornsin K, Kochakarn T, Yeo T, Okombo J, Luth MR, Hoshizaki J, Rawat M, Pearson RD, Schindler KA, Mok S, Park H, Uhlemann AC, Jana GP, Maity BC, Laleu B, Chenu E, Duffy J, Moliner Cubel S, Franco V, Gomez-Lorenzo MG, Gamo FJ, Winzeler EA, Fidock DA, Chookajorn T, Lee MCS. Kümpornsin K, et al. Among authors: duffy j. Nat Commun. 2023 May 27;14(1):3059. doi: 10.1038/s41467-023-38774-1. Nat Commun. 2023. PMID: 37244916 Free PMC article.
1,510 results