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DNDI-6174 is a preclinical candidate for visceral leishmaniasis that targets the cytochrome bc1.
Braillard S, Keenan M, Breese KJ, Heppell J, Abbott M, Islam R, Shackleford DM, Katneni K, Crighton E, Chen G, Patil R, Lee G, White KL, Carvalho S, Wall RJ, Chemi G, Zuccotto F, González S, Marco M, Deakyne J, Standing D, Brunori G, Lyon JJ, Castañeda-Casado P, Camino I, Martinez Martinez MS, Zulfiqar B, Avery VM, Feijens PB, Van Pelt N, Matheeussen A, Hendrickx S, Maes L, Caljon G, Yardley V, Wyllie S, Charman SA, Chatelain E. Braillard S, et al. Among authors: marco m. Sci Transl Med. 2023 Dec 13;15(726):eadh9902. doi: 10.1126/scitranslmed.adh9902. Epub 2023 Dec 13. Sci Transl Med. 2023. PMID: 38091406 Free PMC article.
Short-course combination treatment for experimental chronic Chagas disease.
González S, Wall RJ, Thomas J, Braillard S, Brunori G, Camino Díaz I, Cantizani J, Carvalho S, Castañeda Casado P, Chatelain E, Cotillo I, Fiandor JM, Francisco AF, Grimsditch D, Keenan M, Kelly JM, Kessler A, Luise C, Lyon JJ, MacLean L, Marco M, Martin JJ, Martinez Martinez MS, Paterson C, Read KD, Santos-Villarejo A, Zuccotto F, Wyllie S, Miles TJ, De Rycker M. González S, et al. Among authors: marco m. Sci Transl Med. 2023 Dec 13;15(726):eadg8105. doi: 10.1126/scitranslmed.adg8105. Epub 2023 Dec 13. Sci Transl Med. 2023. PMID: 38091410 Free PMC article.
Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition.
Wyllie S, Brand S, Thomas M, De Rycker M, Chung CW, Pena I, Bingham RP, Bueren-Calabuig JA, Cantizani J, Cebrian D, Craggs PD, Ferguson L, Goswami P, Hobrath J, Howe J, Jeacock L, Ko EJ, Korczynska J, MacLean L, Manthri S, Martinez MS, Mata-Cantero L, Moniz S, Nühs A, Osuna-Cabello M, Pinto E, Riley J, Robinson S, Rowland P, Simeons FRC, Shishikura Y, Spinks D, Stojanovski L, Thomas J, Thompson S, Viayna Gaza E, Wall RJ, Zuccotto F, Horn D, Ferguson MAJ, Fairlamb AH, Fiandor JM, Martin J, Gray DW, Miles TJ, Gilbert IH, Read KD, Marco M, Wyatt PG. Wyllie S, et al. Among authors: marco m. Proc Natl Acad Sci U S A. 2019 May 7;116(19):9318-9323. doi: 10.1073/pnas.1820175116. Epub 2019 Apr 8. Proc Natl Acad Sci U S A. 2019. PMID: 30962368 Free PMC article.
The Qi Site of Cytochrome b is a Promiscuous Drug Target in Trypanosoma cruzi and Leishmania donovani.
Wall RJ, Carvalho S, Milne R, Bueren-Calabuig JA, Moniz S, Cantizani-Perez J, MacLean L, Kessler A, Cotillo I, Sastry L, Manthri S, Patterson S, Zuccotto F, Thompson S, Martin J, Marco M, Miles TJ, De Rycker M, Thomas MG, Fairlamb AH, Gilbert IH, Wyllie S. Wall RJ, et al. Among authors: marco m. ACS Infect Dis. 2020 Mar 13;6(3):515-528. doi: 10.1021/acsinfecdis.9b00426. Epub 2020 Jan 30. ACS Infect Dis. 2020. PMID: 31967783 Free PMC article.
Structure-guided lead optimization of triazolopyrimidine-ring substituents identifies potent Plasmodium falciparum dihydroorotate dehydrogenase inhibitors with clinical candidate potential.
Coteron JM, Marco M, Esquivias J, Deng X, White KL, White J, Koltun M, El Mazouni F, Kokkonda S, Katneni K, Bhamidipati R, Shackleford DM, Angulo-Barturen I, Ferrer SB, Jiménez-Díaz MB, Gamo FJ, Goldsmith EJ, Charman WN, Bathurst I, Floyd D, Matthews D, Burrows JN, Rathod PK, Charman SA, Phillips MA. Coteron JM, et al. Among authors: marco m. J Med Chem. 2011 Aug 11;54(15):5540-61. doi: 10.1021/jm200592f. Epub 2011 Jul 14. J Med Chem. 2011. PMID: 21696174 Free PMC article.
Tetrahydro-2-naphthyl and 2-Indanyl Triazolopyrimidines Targeting Plasmodium falciparum Dihydroorotate Dehydrogenase Display Potent and Selective Antimalarial Activity.
Kokkonda S, Deng X, White KL, Coteron JM, Marco M, de Las Heras L, White J, El Mazouni F, Tomchick DR, Manjalanagara K, Rudra KR, Chen G, Morizzi J, Ryan E, Kaminsky W, Leroy D, Martínez-Martínez MS, Jimenez-Diaz MB, Bazaga SF, Angulo-Barturen I, Waterson D, Burrows JN, Matthews D, Charman SA, Phillips MA, Rathod PK. Kokkonda S, et al. Among authors: marco m. J Med Chem. 2016 Jun 9;59(11):5416-31. doi: 10.1021/acs.jmedchem.6b00275. Epub 2016 May 21. J Med Chem. 2016. PMID: 27127993 Free PMC article.
Antitrypanosomal 8-Hydroxy-Naphthyridines Are Chelators of Divalent Transition Metals.
Wall RJ, Moniz S, Thomas MG, Norval S, Ko EJ, Marco M, Miles TJ, Gilbert IH, Horn D, Fairlamb AH, Wyllie S. Wall RJ, et al. Among authors: marco m. Antimicrob Agents Chemother. 2018 Jul 27;62(8):e00235-18. doi: 10.1128/AAC.00235-18. Print 2018 Aug. Antimicrob Agents Chemother. 2018. PMID: 29844044 Free PMC article.
Identification and Optimization of a Series of 8-Hydroxy Naphthyridines with Potent In Vitro Antileishmanial Activity: Initial SAR and Assessment of In Vivo Activity.
Thomas MG, De Rycker M, Wall RJ, Spinks D, Epemolu O, Manthri S, Norval S, Osuna-Cabello M, Patterson S, Riley J, Simeons FRC, Stojanovski L, Thomas J, Thompson S, Naylor C, Fiandor JM, Wyatt PG, Marco M, Wyllie S, Read KD, Miles TJ, Gilbert IH. Thomas MG, et al. Among authors: marco m. J Med Chem. 2020 Sep 10;63(17):9523-9539. doi: 10.1021/acs.jmedchem.0c00705. Epub 2020 Aug 13. J Med Chem. 2020. PMID: 32663005 Free PMC article.
Scaffold-Hopping Strategy on a Series of Proteasome Inhibitors Led to a Preclinical Candidate for the Treatment of Visceral Leishmaniasis.
Thomas M, Brand S, De Rycker M, Zuccotto F, Lukac I, Dodd PG, Ko EJ, Manthri S, McGonagle K, Osuna-Cabello M, Riley J, Pont C, Simeons F, Stojanovski L, Thomas J, Thompson S, Viayna E, Fiandor JM, Martin J, Wyatt PG, Miles TJ, Read KD, Marco M, Gilbert IH. Thomas M, et al. Among authors: marco m. J Med Chem. 2021 May 13;64(9):5905-5930. doi: 10.1021/acs.jmedchem.1c00047. Epub 2021 Apr 27. J Med Chem. 2021. PMID: 33904304 Free PMC article.
Structure-Guided Design and Synthesis of a Pyridazinone Series of Trypanosoma cruzi Proteasome Inhibitors.
Thomas MG, McGonagle K, Rowland P, Robinson DA, Dodd PG, Camino-Díaz I, Campbell L, Cantizani J, Castañeda P, Conn D, Craggs PD, Edwards D, Ferguson L, Fosberry A, Frame L, Goswami P, Hu X, Korczynska J, MacLean L, Martin J, Mutter N, Osuna-Cabello M, Paterson C, Peña I, Pinto EG, Pont C, Riley J, Shishikura Y, Simeons FRC, Stojanovski L, Thomas J, Wrobel K, Young RJ, Zmuda F, Zuccotto F, Read KD, Gilbert IH, Marco M, Miles TJ, Manzano P, De Rycker M. Thomas MG, et al. Among authors: marco m. J Med Chem. 2023 Aug 10;66(15):10413-10431. doi: 10.1021/acs.jmedchem.3c00582. Epub 2023 Jul 28. J Med Chem. 2023. PMID: 37506194 Free PMC article.
1,404 results