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  • 2020
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  • Susan Wyllie
Article

8-Alkynyl-3-nitroimidazopyridines display potent antitrypanosomal activity against both T. b. brucei and cruzi

Fersing, C., Boudot, C., Castera-Ducros, C., Pinault, E., Hutter, S., Paoli-Lombardo, R., Primas, N., Pedron, J., Seguy, L., Bourgeade-Delmas, S., Sournia-Saquet, A., Stigliani, J. L., Brossas, J. Y., Paris, L., Valentin, A., Wyllie, S., Fairlamb, A. H., Boutet-Robinet, É., Corvaisier, S., Since, M. & 8 others, Malzert-Fréon, A., Destere, A., Mazier, D., Rathelot, P., Courtioux, B., Azas, N., Verhaeghe, P. & Vanelle, P., 15 Sep 2020, In : European Journal of Medicinal Chemistry. 202, 15 p., 112558.

Research output: Contribution to journalArticle

8-Aryl-6-chloro-3-nitro-2-(phenylsulfonylmethyl)imidazo[1,2-a]pyridines as potent antitrypanosomatid molecules bioactivated by type 1 nitroreductases

Fersing, C., Boudot, C., Pedron, J., Hutter, S., Primas, N., Castera-Ducros, C., Bourgeade-Delmas, S., Sournia-Saquet, A., Moreau, A., Cohen, A., Stigliani, J-L., Pratviel, G., Crozet, M. D., Wyllie, S., Fairlamb, A., Valentin, A., Rathelot, P., Azas, N., Courtioux, B., Verhaeghe, P. & 1 others, Vanelle, P., 5 Sep 2018, In : European Journal of Medicinal Chemistry. 157, p. 115-126 12 p.

Research output: Contribution to journalArticle

Open Access
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6 Citations (Scopus)
7 Downloads (Pure)

Activation of bicyclic nitro-drugs by a novel nitroreductase (NTR2) in Leishmania

Wyllie, S., Roberts, A. J., Norval, S., Patterson, S., Foth, B. J., Berriman, M., Read, K. D. & Fairlamb, A. H., 3 Nov 2016, In : PLoS Pathogens. 12, 11, p. 1-22 22 p., e1005971.

Research output: Contribution to journalArticle

Open Access
File
34 Citations (Scopus)
150 Downloads (Pure)

Antikinetoplastid SAR study in 3-nitroimidazopyridine series: identification of a novel non-genotoxic and potent anti-T. b. brucei hit-compound with improved pharmacokinetic properties.

Fersing, C., Boudot, C., Paoli-Lombardo, R., Primas, N., Pinault, E., Hutter, S., Castera-Ducros, C., Kabri, Y., Pedron, J., Bourgeade-Delmas, S., Sournia-Saquet, A., Stigliani, J. L., Valentin, A., Azqueta, A., Muruzabal, D., Destere, A., Wyllie, S., Fairlamb, A. H., Corvaisier, S., Since, M. & 7 others, Malzert-Fréon, A., Di Giorgio, C., Rathelot, P., Azas, N., Courtioux, B., Vanelle, P. & Verhaeghe, P., 4 Aug 2020, In : European Journal of Medicinal Chemistry. 206, 20 p., 112668.

Research output: Contribution to journalArticle

Anti-trypanosomal 8-hydroxyl naphthyridines are chelators of divalent transition metals

Wall, R. J., Moniz, S., Thomas, M., Norval, S., Ko, E. J., Marco, M., Miles, T. J., Gilbert, I., Horn, D., Fairlamb, A. & Wyllie, S., Aug 2018, In : Antimicrobial Agents and Chemotherapy. 62, 8, p. 1-15 15 p., e00235-18.

Research output: Contribution to journalArticle

Open Access
File
3 Citations (Scopus)
169 Downloads (Pure)

Antitrypanosomatid Pharmacomodulation at Position 3 of the 8-Nitroquinolin-2(1H)-one Scaffold Using Palladium-Catalysed Cross-Coupling Reactions

Pedron, J., Boudot, C., Bourgeade-Delmas, S., Sournia-Saquet, A., Paloque, L., Rastegari, M., Abdoulaye, M., El-Kashef, H., Bonduelle, C., Pratviel, G., Wyllie, S., Fairlamb, A. H., Courtioux, B., Verhaeghe, P. & Valentin, A., 22 Oct 2018, In : ChemMedChem. 13, 20, p. 2217-2228 12 p.

Research output: Contribution to journalArticle

Open Access
File
5 Citations (Scopus)
89 Downloads (Pure)

Clinical and veterinary trypanocidal benzoxaboroles target CPSF3

Wall, R., Rico Vidal, E., Lukac, I., Zuccotto, F., Elg, S., Gilbert, I., Freund, Y. R., Alley, M. R. K., Field, M., Wyllie, S. & Horn, D., 18 Sep 2018, In : Proceedings of the National Academy of Sciences of the United States of America. 115, 38, p. 9616-9621 6 p.

Research output: Contribution to journalArticle

Open Access
File
19 Citations (Scopus)
274 Downloads (Pure)

Cyclin-dependent kinase 12 is a drug target for visceral leishmaniasis

Wyllie, S., Thomas, M., Patterson, S., Crouch, S., De Rycker, M., Lowe, R., Gresham, S., Urbaniak, M. D., Otto, T. D., Stojanovski, L., Simeons, F. R. C., Manthri, S., MacLean, L. M., Zuccotto, F., Homeyer, N., Pflaumer, H., Boesche, M., Sastry, L., Connolly, P., Albrecht, S. & 12 others, Berriman, M., Drewes, G., Gray, D. W., Ghidelli-Disse, S., Dixon, S., Fiandor, J. M., Wyatt, P. G., Ferguson, M. A. J., Fairlamb, A. H., Miles, T. J., Read, K. D. & Gilbert, I. H., 9 Aug 2018, In : Nature. 560, 7717, p. 192-197 6 p.

Research output: Contribution to journalArticle

Open Access
File
37 Citations (Scopus)
503 Downloads (Pure)

Development of chemical proteomics for the folateome and analysis of the kinetoplastid folateome

Webster, L., Thomas, M., Urbaniak, M., Wyllie, S., Ong, H., Tinti, M., Fairlamb, A., Boesche, M., Ghidelli-Disse, S., Drewes, G. & Gilbert, I., 12 Oct 2018, In : ACS Infectious Diseases. 4, 10, p. 1475-1486 12 p.

Research output: Contribution to journalArticle

Open Access
File
143 Downloads (Pure)

New 8-nitroquinolinone derivative displaying submicromolar in vitro activities against both Trypanosoma brucei and cruzi

Pedron, J., Boudot, C., Brossas, J., Pinault, E., Bourgeade-Delmas, S., Sournia-Saquet, A., Boutet-Robinet, E., Destere, A., Tronnet, A., Bergé, J., Bonduelle, C., Deraeve, C., Pratviel, G., Stigliani, J-L., Paris, L., Mazier, D., Corvaisier, S., Since, M., Malzert-Freon, A., Wyllie, S. & 5 others, Milne, R., Fairlamb, A. H., Valentin, A., Courtioux, B. & Verhaeghe, P., 9 Apr 2020, In : ACS Medicinal Chemistry Letters. 11, 4, p. 464-472 9 p.

Research output: Contribution to journalArticle

Open Access
File
40 Downloads (Pure)

Nitroheterocyclic drug resistance mechanisms in Trypanosoma brucei

Wyllie, S., Foth, B. J., Kelner, A., Sokolova, A. Y., Berriman, M. & Fairlamb, A., Mar 2016, In : Journal of Antimicrobial Chemotherapy. 71, 3, p. 625-634 10 p.

Research output: Contribution to journalArticle

Open Access
File
40 Citations (Scopus)
183 Downloads (Pure)

Nongenotoxic 3-Nitroimidazo[1,2-a]pyridines Are NTR1 Substrates That Display Potent in Vitro Antileishmanial Activity

Fersing, C., Basmaciyan, L., Boudot, C., Pedron, J., Hutter, S., Cohen, A., Castera-Ducros, C., Primas, N., Laget, M., Casanova, M., Bourgeade-Delmas, S., Piednoel, M., Sournia-Saquet, A., Belle Mbou, V., Courtioux, B., Boutet-Robinet, É., Since, M., Milne, R., Wyllie, S., Fairlamb, A. H. & 5 others, Valentin, A., Rathelot, P., Verhaeghe, P., Vanelle, P. & Azas, N., 10 Jan 2019, In : ACS Medicinal Chemistry Letters. 10, 1, p. 34-39 6 p.

Research output: Contribution to journalArticle

Open Access
File
8 Citations (Scopus)
206 Downloads (Pure)

Novel 8-nitroquinolin-2(1H)-ones as NTR-bioactivated antikinetoplastid molecules: Synthesis, electrochemical and SAR study

Pedron, J., Boudot, C., Hutter, S., Bourgeade-Delmas, S., Stigliani, J-L., Sournia-Saquet, A., Moreau, A., Boutet-Robinet, E., Paloque, L., Mothes, E., Laget, M., Vendier, L., Pratviel, G., Wyllie, S., Fairlamb, A., Azas, N., Courtioux, B., Valentin, A. & Verhaeghe, P., 15 Jul 2018, In : European Journal of Medicinal Chemistry. 155, p. 135-152 18 p.

Research output: Contribution to journalArticle

Open Access
File
8 Citations (Scopus)
152 Downloads (Pure)

Pentacyclic nitrofurans that rapidly kill nifurtimox-resistant trypanosomes

Bruhn, D. F., Wyllie, S., Rodríguez-Cortés, A., Carrillo, A. K., Rakesh, Guy, R. K., Fairlamb, A. H. & Lee, R. E., Apr 2016, In : Journal of Antimicrobial Chemotherapy. 71, 4, p. 956-963 8 p., dkv417.

Research output: Contribution to journalArticle

5 Citations (Scopus)
Open Access
File
11 Citations (Scopus)
183 Downloads (Pure)

Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition

Wyllie, S., Brand, S., Thomas, M., De Rycker, M., Chung, C-W., Peña, I., Bingham, R., Bueren-Calabuig, J., Cantizani, J., Cebrian, D., Craggs, P. D., Ferguson, L., Goswami, P., Hobrath, J., Howe, J., Jeacock, L., Ko, E. J., Korczynska, J., MacLean, L., Manthri, S. & 29 others, Santos Martinez, M., Mata-Cantero, L., Moniz, S., Nuhs, A., Osuna-Cabello, M., Pinto, E., Riley, J., Robinson, S., Rowland, P., Simeons, F., Shishikura, Y., Spinks, D., Stojanovski, L., Thomas, J., Thompson, S., Viayna Gaza, E., Wall, R., Zuccotto, F., Horn, D., Ferguson, M., Fairlamb, A., Fiandor, J. M., Martín, J., Gray, D., Miles, T. J., Gilbert, I., Read, K., Marco, M. & Wyatt, P., 7 May 2019, In : Proceedings of the National Academy of Sciences. 116, 19, p. 9318-9323 6 p., 201820175.

Research output: Contribution to journalArticle

Open Access
File
25 Citations (Scopus)
143 Downloads (Pure)

Setting our sights on infectious diseases

De Rycker, M., Horn, D., Aldridge, B., Amewu, R. K., Barry, C. E., Buckner, F. S., Cook, S., Ferguson, M. A. J., Gobeau, N., Herrmann, J., Herrling, P., Hope, W., Keiser, J., Lafuente-Monasterio, M. J., Leeson, P. D., Leroy, D., Manjunatha, U. H., McCarthy, J., Miles, T. J., Mizrahi, V. & 17 others, Moshynets, O., Niles, J., Overington, J. P., Pottage, J., Rao, S. P. S., Read, K. D., Ribeiro, I., Silver, L. L., Southern, J., Spangenberg, T., Sundar, S., Taylor, C., Van Voorhis, W. C., White, N. J., Wyllie, S., Wyatt, P. G. & Gilbert, I. H., 10 Jan 2020, In : ACS Infectious Diseases. 6, p. 3-13 11 p.

Research output: Contribution to journalArticle

Open Access
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70 Downloads (Pure)

The anti-tubercular drug delamanid as a potential oral treatment for visceral leishmaniasis

Patterson, S., Wyllie, S., Norval, S., Stojanovski, L., Simeons, F. R. C., Auer, J. L., Osuna-Cabello, M., Read, K. D. & Fairlamb, A. H., 24 May 2016, In : eLife. 5, p. 1-21 21 p., e09744.

Research output: Contribution to journalArticle

Open Access
File
41 Citations (Scopus)
194 Downloads (Pure)

The Qi Site of Cytochrome b is a Promiscuous Drug Target in Trypanosoma cruzi and Leishmania donovani: ACS Infectious Diseases

Wall, R. J., Carvalho, S., Milne, R., Bueren-Calabuig, J. A., 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, T. J., De Rycker, M., Thomas, M. G., Fairlamb, A. H. & 2 others, Gilbert, I. H. & Wyllie, S., 13 Mar 2020, In : ACS Infectious Diseases. 6, 3, p. 515-528 14 p.

Research output: Contribution to journalArticle

Open Access
File
2 Citations (Scopus)
45 Downloads (Pure)