1991 …2024

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Article
2020

An in vitro toolbox to accelerate anti-malarial drug discovery and development

Charman, S. A., Andreu, A., Barker, H., Blundell, S., Campbell, A., Campbell, M., Chen, G., Chiu, F. C. K., Crighton, E., Katneni, K., Morizzi, J., Patil, R., Pham, T., Ryan, E., Saunders, J., Shackleford, D. M., White, K. L., Almond, L., Dickins, M., Smith, D. A. & 3 others, Moehrle, J. J., Burrows, J. N. & Abla, N., 2 Jan 2020, In : Malaria Journal. 19, 1, 27 p., 1.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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1 Citation (Scopus)
2019

3,3′-Disubstituted 5,5′-Bi(1,2,4-triazine) Derivatives with Potent in Vitro and in Vivo Antimalarial Activity

Xue, L., Shi, D. H., Harjani, J. R., Huang, F., Beveridge, J. G., Dingjan, T., Ban, K., Diab, S., Duffy, S., Lucantoni, L., Fletcher, S., Chiu, F. C. K., Blundell, S., Ellis, K., Ralph, S. A., Wirjanata, G., Teguh, S., Noviyanti, R., Chavchich, M., Creek, D. & 10 others, Price, R. N., Marfurt, J., Charman, S. A., Cuellar, M. E., Strasser, J. M., Dahlin, J. L., Walters, M. A., Edstein, M. D., Avery, V. M. & Baell, J. B., 1 Jan 2019, In : Journal of Medicinal Chemistry. 62, 5, p. 2485-2498 14 p.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

Discovery of benzoylsulfonohydrazides as potent inhibitors of the histone acetyltransferase KAT6A

Leaver, D. J., Cleary, B., Nguyen, N., Priebbenow, D., Lagiakos, H. R., Sanchez, J., Xue, L., Huang, F., Sun, Y., Mujumdar, P., Mudududdla, R., Varghese, S., Teguh, S., Charman, S. A., White, K. L., Katneni, K., Cuellar, M., Strasser, J. M., Dahlin, J. L., Walters, M. A. & 10 others, Street, I. P., Monahan, B. J., Jarman, K. E., Sabroux, H. J., Falk, H., Chung, M. C., Hermans, S. J., Parker, M. W., Thomas, T. & Baell, J. B., 8 Aug 2019, In : Journal of Medicinal Chemistry. 62, 15, p. 7146-7159 14 p.

Research output: Contribution to journalArticleResearchpeer-review

3 Citations (Scopus)

Evaluation of 4-amino 2-anilinoquinazolines against Plasmodium and other apicomplexan parasites in vitro and in a P. Falciparum Humanized NOD-scid IL2R null Mouse Model of Malaria

Gilson, P. R., Nguyen, W., Poole, W. A., Teixeira, J. E., Thompson, J. K., Guo, K., Stewart, R. J., Ashton, T. D., White, K. L., Sanz, L. M., Gamo, F. J., Charman, S. A., Wittlin, S., Duffy, J., Tonkin, C. J., Tham, W. H., Crabb, B. S., Cooke, B. M., Huston, C. D., Cowman, A. F. & 1 others, Sleebs, B. E., 1 Mar 2019, In : Antimicrobial Agents and Chemotherapy. 63, 3, 15 p., e01804-18.

Research output: Contribution to journalArticleResearchpeer-review

Falcipain Inhibitors Based on the Natural Product Gallinamide A Are Potent in Vitro and in Vivo Antimalarials

Stoye, A., Juillard, A., Tang, A. H., Legac, J., Gut, J., White, K. L., Charman, S. A., Rosenthal, P. J., Grau, G. E. R., Hunt, N. H. & Payne, R. J., 13 Jun 2019, In : Journal of Medicinal Chemistry. 62, 11, p. 5562-5578 17 p.

Research output: Contribution to journalArticleResearchpeer-review

6 Citations (Scopus)

Inhibition of cytomegalovirus replication with extended-half-life synthetic ozonides

Wang, Y., Mukhopadhyay, R., Roy, S., Kapoor, A., Su, Y. P., Charman, S. A., Chen, G., Wu, J., Wang, X., Vennerstrom, J. L. & Arav-Boger, R., 1 Jan 2019, In : Antimicrobial Agents and Chemotherapy. 63, 1, 14 p., e01735-18.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

Novel Human Aminopeptidase N Inhibitors: Discovery and Optimization of Subsite Binding Interactions

Lee, J., Vinh, N. B., Drinkwater, N., Yang, W., Kannan Sivaraman, K., Schembri, L. S., Gazdik, M., Grin, P. M., Butler, G. S., Overall, C. M., Charman, S. A., McGowan, S. & Scammells, P. J., 8 Aug 2019, In : Journal of Medicinal Chemistry. 62, 15, p. 7185-7209 25 p.

Research output: Contribution to journalArticleResearchpeer-review

4 Citations (Scopus)

Ozonide Antimalarials Alkylate Heme in the Malaria Parasite Plasmodium falciparum

Giannangelo, C., Anderson, D., Wang, X., Vennerstrom, J. L., Charman, S. A. & Creek, D. J., 17 Oct 2019, In : ACS Infectious Diseases. 5, 12, p. 2076-2086 11 p.

Research output: Contribution to journalArticleResearchpeer-review

3 Citations (Scopus)

The Development Process for Discovery and Clinical Advancement of Modern Antimalarials

Ashton, T. D., Devine, S., Mohrle, J., Laleu, B., Burrows, J. N., Charman, S., Creek, D. & Sleebs, B. E., 6 Aug 2019, In : Journal of Medicinal Chemistry. 62, 23, p. 10526-10562 37 p.

Research output: Contribution to journalArticleResearchpeer-review

2 Citations (Scopus)
2018

Assessing drug efficacy against Plasmodium falciparum liver stages in vivo

Flannery, E. L., Foquet, L., Chuenchob, V., Fishbaugher, M., Billman, Z., Navarro, M. J., Betz, W., Olsen, T. M., Lee, J., Camargo, N., Nguyen, T., Schafer, C., Sack, B. K., Wilson, E. M., Saunders, J., Bial, J., Campo, B., Charman, S. A., Murphy, S. C., Phillips, M. A. & 2 others, Kappe, S. H. & Mikolajczak, S. A., 11 Jan 2018, In : JCI Insight. 3, 1, 12 p., e92587.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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6 Citations (Scopus)

Derivatives of a benzoquinone acyl hydrazone with activity against Toxoplasma gondii

Sanford, A. G., Schulze, T. T., Potluri, L. P., Watson, G. F., Darner, E. B., Zach, S. J., Hemsley, R. M., Wallick, A. I., Warner, R. C., Charman, S. A., Wang, X., Vennerstrom, J. L. & Davis, P. H., 1 Dec 2018, In : International Journal for Parasitology: Drugs and Drug Resistance. 8, 3, p. 488-492 5 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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2 Citations (Scopus)

Isoxazolopyrimidine-Based Inhibitors of Plasmodium falciparum Dihydroorotate Dehydrogenase with Antimalarial Activity

Kokkonda, S., El Mazouni, F., White, K. L., White, J., Shackleford, D. M., Lafuente-Monasterio, M. J., Manjalanagara, K., Joseph, J. T., Garcia-Pérez, A., Fernandez, J., Gamo, F. J., Waterson, D., Burrows, J. N., Palmer, M. J., Charman, S. A., Rathod, P. K. & Phillips, M. A., Aug 2018, In : ACS Omega. 3, 8, p. 9227-9240 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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6 Citations (Scopus)

Novel Toxoplasma gondii inhibitor chemotypes

Sanford, A. G., Schulze, T. T., Potluri, L. P., Hemsley, R. M., Larson, J. J., Judge, A. K., Zach, S. J., Wang, X., Charman, S. A., Vennerstrom, J. L. & Davis, P. H., 1 Apr 2018, In : Parasitology International. 67, 2, p. 107-111 5 p.

Research output: Contribution to journalArticleResearchpeer-review

6 Citations (Scopus)

Parasite-mediated degradation of synthetic ozonide antimalarials impacts in vitro antimalarial activity

Giannangelo, C., Stingelin, L., Yang, T., Tilley, L., Charman, S. A. & Creek, D. J., 1 Mar 2018, In : Antimicrobial Agents and Chemotherapy. 62, 3, 14 p., e01566-17.

Research output: Contribution to journalArticleResearchpeer-review

5 Citations (Scopus)

Progress in antischistosomal N,N′-diaryl urea SAR

Wu, J., Wang, C., Leas, D., Vargas, M., White, K. L., Shackleford, D. M., Chen, G., Sanford, A. G., Hemsley, R. M., Davis, P. H., Dong, Y., Charman, S. A., Keiser, J. & Vennerstrom, J. L., 1 Feb 2018, In : Bioorganic and Medicinal Chemistry Letters. 28, 3, p. 244-248 5 p.

Research output: Contribution to journalArticleResearchpeer-review

4 Citations (Scopus)

SAR of a new antischistosomal urea carboxylic acid

Wu, J., Wang, C., Häberli, C., White, K. L., Shackleford, D. M., Chen, G., Dong, Y., Charman, S. A., Keiser, J. & Vennerstrom, J. L., 15 Dec 2018, In : Bioorganic and Medicinal Chemistry Letters. 28, 23-24, p. 3648-3651 4 p.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria

O’ Neill, P. M., Stocks, P. A., Sabbani, S., Roberts, N. L., Amewu, R. K., Shore, E. R., Aljayyoussi, G., Angulo-Barturén, I., Belén, M., Jiménez-Díaz, Bazaga, S. F., Martínez, M. S., Campo, B., Sharma, R., Charman, S. A., Ryan, E., Chen, G., Shackleford, D. M., Davies, J., Nixon, G. L. & 2 others, Biagini, G. A. & Ward, S. A., 15 Jul 2018, In : Bioorganic & Medicinal Chemistry. 26, 11, p. 2996-3005 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Uct943, a next-generation Plasmodium falciparum pi4k inhibitor preclinical candidate for the treatment of malaria

Brunschwig, C., Lawrence, N., Taylor, D., Abay, E., Njoroge, M., Basarab, G. S., Le Manach, C., Paquet, T., Cabrera, D. G., Nchinda, A. T., De Kock, C., Wiesner, L., Denti, P., Waterson, D., Blasco, B., Leroy, D., Witty, M. J., Donini, C., Duffy, J., Wittlin, S. & 28 others, White, K. L., Charman, S. A., Jiménez-Díaz, M. B., Angulo-Barturen, I., Herreros, E., Gamo, F. J., Rochford, R., Mancama, D., Coetzer, T. L., Van der Watt, M. E., Reader, J., Birkholtz, L. M., Marsh, K. C., Solapure, S. M., Burke, J. E., McPhail, J. A., Vanaerschot, M., Fidock, D. A., Fish, P. V., Siegl, P., Smith, D. A., Wirjanata, G., Noviyanti, R., Price, R. N., Marfurt, J., Silue, K. D., Street, L. J. & Chibaleb, K., 1 Sep 2018, In : Antimicrobial Agents and Chemotherapy. 62, 9, 16 p., e00012-18.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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10 Citations (Scopus)

Using Human Plasma as an Assay Medium in Caco-2 Studies Improves Mass Balance for Lipophilic Compounds

Katneni, K., Pham, T., Saunders, J., Chen, G., Patil, R., White, K. L., Abla, N., Chiu, F. C. K., Shackleford, D. M. & Charman, S. A., 1 Nov 2018, In : Pharmaceutical Research. 35, 11, 13 p., 210.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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2 Citations (Scopus)
2017

Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase

Paquet, T., Le Manach, C., Cabrera, D. G., Younis, Y., Henrich, P. P., Abraham, T. S., Lee, M. C. S., Basak, R., Ghidelli-Disse, S., Lafuente-Monasterio, M. J., Bantscheff, M., Ruecker, A., Blagborough, A. M., Zakutansky, S. E., Zeeman, A-M., White, K. L., Shackleford, D. M., Mannila, J., Morizzi, J., Scheurer, C. & 1 others, Charman, S. A., 26 Apr 2017, In : Science Translational Medicine. 9, 387, 14 p., eaad9735.

Research output: Contribution to journalArticleResearchpeer-review

70 Citations (Scopus)

Antimalarial Inhibitors Targeting Serine Hydroxymethyltransferase (SHMT) with in Vivo Efficacy and Analysis of their Binding Mode Based on X-ray Cocrystal Structures

Schwertz, G., Witschel, M. C., Rottmann, M., Bonnert, R., Leartsakulpanich, U., Chitnumsub, P., Jaruwat, A., Ittarat, W., Schäfer, A., Aponte, R. A., Charman, S. A., White, K. L., Kundu, A., Sadhukhan, S., Lloyd, M., Freiberg, G. M., Srikumaran, M., Siggel, M., Zwyssig, A., Chaiyen, P. & 1 others, Diederich, F., 22 Jun 2017, In : Journal of Medicinal Chemistry. 60, 12, p. 4840-4860 21 p.

Research output: Contribution to journalArticleResearchpeer-review

13 Citations (Scopus)

A tetraoxane-based antimalarial drug candidate that overcomes PfK13-C580Y dependent artemisinin resistance

O'Neill, P. M., Amewu, R. K., Charman, S. A., Sabbani, S., Gnädig, N. F., Straimer, J., Fidock, D. A., Shore, E. R., Roberts, N. L., Wong, M. H. L., Hong, W. D., Pidathala, C., Riley, C., Murphy, B., Aljayyoussi, G., Gamo, F. J., Sanz, L., Rodrigues, J., Cortes, C. G., Herreros, E. & 2 others, Ryan, E. & Shackleford, D. M., 24 May 2017, In : Nature Communications. 8, 10 p., 15159.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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27 Citations (Scopus)

Long-Lasting and Fast-Acting in Vivo Efficacious Antiplasmodial Azepanylcarbazole Amino Alcohol

Abla, N., Bashyam, S., Charman, S. A., Greco, B., Hewitt, P., Jiménez-Díaz, M. B., Katneni, K., Kubas, H., Picard, D., Sambandan, Y., Sanz, L., Smith, D., Wang, T., Willis, P., Wittlin, S. & Spangenberg, T., 14 Dec 2017, In : ACS Medicinal Chemistry Letters. 8, 12, p. 1304-1308 5 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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1 Citation (Scopus)

Novel inhibitors of Plasmodium falciparum based on 2,5-disubstituted furans

Krake, S. H., Martinez, P. D. G., McLaren, J., Ryan, E., Chen, G., White, K., Charman, S. A., Campbell, S., Willis, P. & Dias, L. C., 27 Jan 2017, In : European Journal of Medicinal Chemistry. 126, p. 929-936 8 p.

Research output: Contribution to journalArticleResearchpeer-review

7 Citations (Scopus)

Sansanmycin natural product analogues as potent and selective anti-mycobacterials that inhibit lipid I biosynthesis

Tran, A. T., Watson, E. E., Pujari, V., Conroy, T., Dowman, L. J., Giltrap, A. M., Pang, A., Wong, W. R., Linington, R. G., Mahapatra, S., Saunders, J., Charman, S. A., West, N. P., Bugg, T. D. H., Tod, J., Dowson, C. G., Roper, D. I., Crick, D. C., Britton, W. J. & Payne, R. J., 1 Mar 2017, In : Nature Communications. 8, 9 p., 14414.

Research output: Contribution to journalArticleResearchpeer-review

File
15 Citations (Scopus)

Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439)

Dong, Y., Wang, X., Kamaraj, S., Bulbule, V. J., Chiu, F. C. K., Chollet, J., Dhanasekaran, M., Hein, C. D., Papastogiannidis, P., Morizzi, J., Shackleford, D. M., Barker, H., Ryan, E., Scheurer, C., Tang, Y., Zhao, Q., Zhou, L., White, K. L., Urwyler, H., Charman, W. N. & 4 others, Matile, H., Wittlin, S., Charman, S. A. & Vennerstrom, J. L., 13 Apr 2017, In : Journal of Medicinal Chemistry. 60, 7, p. 2654-2668 15 p.

Research output: Contribution to journalArticleResearchpeer-review

21 Citations (Scopus)

The novel compound PBT434 prevents iron mediated neurodegeneration and alpha-synuclein toxicity in multiple models of Parkinson’s disease

Finkelstein, D. I., Billings, J. L., Adlard, P. A., Ayton, S., Sedjahtera, A., Masters, C. L., Wilkins, S., Shackleford, D., Charman, S. A., Bal, W., Zawisza, I. A., Kurowska, E., Gundlach, A. L., Ma, S., Bush, A. I., Hare, D. J., Doble, P. A., Crawford, S. A., Gautier, E. C., Parsons, J. & 3 others, Huggins, P., Barnham, K. J. & Cherny, R. A., 28 Jun 2017, In : Acta neuropathologica communications. 5, 1, 16 p., 53.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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22 Citations (Scopus)
2016

A triazolopyrimidine-based dihydroorotate dehydrogenase inhibitor with improved drug-like properties for treatment and prevention of malaria

Phillips, M. A., White, K., Kokkonda, S., Deng, X., White, J., El Mazouni, F., Marsh, K., Tomchick, D. R., Manjalanagara, K., Rudra, K. R., Wirjanata, G., Noviyanti, R., Price, R. N., Marfurt, J., Shackleford, D., Chiu, F., Campbell, M., Jimenez-Diaz, M. B., Bazaga, S. F., Angulo-Barturen, I. & 1 others, Charman, S., 9 Dec 2016, In : ACS Infectious Diseases. 2, 12, p. 945-957 13 p.

Research output: Contribution to journalArticleResearchpeer-review

38 Citations (Scopus)

Comparison of the exposure time dependence of the activities of synthetic ozonide antimalarials and dihydroartemisinin against K13 wild-type and mutant Plasmodium falciparum strains

Yang, T., Xie, S. C., Cao, P., Giannangelo, C., McCaw, J., Creek, D. J., Charman, S. A., Klonis, N. & Tilley, L., 1 Aug 2016, In : Antimicrobial Agents and Chemotherapy. 60, 8, p. 4501-4510 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
25 Citations (Scopus)

Haemoglobin degradation underpins the sensitivity of early ring stage Plasmodium falciparum to artemisinins

Xie, S. C., Dogovski, C., Hanssen, E., Chiu, F., Yang, T., Crespo, M. P., Stafford, C., Batinovic, S., Teguh, S., Charman, S., Klonis, N. & Tilley, L., 2016, In : Journal of Cell Science. 129, 2, p. 406-416 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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42 Citations (Scopus)

Hit-to-lead optimization of a novel class of potent, broad-spectrum trypanosomacides

Russell, S., Rahmani, R., Jones, A. J., Newson, H. L., Neilde, K., Cotillo, I., Rahmani Khajouei, M., Ferrins, L., Qureishi, S., Nguyen, N., Martinez-Martinez, M. S., Weaver, D. F., Kaiser, M., Riley, J., Thomas, J., De Rycker, M., Read, K. D., Flematti, G. R., Ryan, E., Tanghe, S. & 6 others, Rodriguez, A., Charman, S. A., Kessler, A., Avery, V. M., Baell, J. B. & Piggott, M. J., 10 Nov 2016, In : Journal of Medicinal Chemistry. 59, 21, p. 9686-9720 35 p.

Research output: Contribution to journalArticleResearchpeer-review

17 Citations (Scopus)

Identification of a potential antimalarial drug candidate from a series of 2-aminopyrazines by optimization of aqueous solubility and potency across the parasite life cycle

Le Manach, C., Nchinda, A. T., Paquet, T., Gonzàlez Cabrera, D., Younis, Y., Han, Z., Bashyam, S., Zabiulla, M., Taylor, D., Lawrence, N., White, K. L., Charman, S. A., Waterson, D., Witty, M. J., Wittlin, S., Botha, M. E., Nondaba, S. H., Reader, J., Birkholtz, L. M. & Jiménez-Díaz, M. B., 10 Nov 2016, In : Journal of Medicinal Chemistry. 59, 21, p. 9890-9905 16 p.

Research output: Contribution to journalArticleResearchpeer-review

25 Citations (Scopus)

Nitroheterocyclic drugs cure experimental Trypanosoma cruzi infections more effectively in the chronic stage than in the acute stage

Francisco, A. F., Jayawardhana, S., Lewis, M. D., White, K. L., Shackleford, D. M., Chen, G., Saunders, J., Osuna-Cabello, M., Read, K. D., Charman, S. A., Chatelain, E. & Kelly, J. M., 17 Oct 2016, In : Scientific Reports. 6, 11 p., 35351.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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29 Citations (Scopus)

Open source drug discovery: Highly potent antimalarial compounds derived from the tres cantos arylpyrroles

Williamson, A. E., Ylioja, P. M., Robertson, M. N., Antonova-Koch, Y., Avery, V., Baell, J., Batchu, H., Batra, S., Burrows, J. N., Bhattacharyya, S., Calderon, F., Charman, S., Clark, J., Crespo, B., Dean, M., Debbert, S. L., Delves, M. J., Dennis, A. S. M., Deroose, F., Duffy, S. & 3 others, Ryan, E., Wells, T. & White, K., 26 Oct 2016, In : ACS Central Science. 2, 10, p. 687-701 15 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
29 Citations (Scopus)

Potent dual inhibitors of Plasmodium falciparum M1 and M17 aminopeptidases through optimization of S1 pocket interactions

Drinkwater, N., Vinh, N. B., Mistry, S. N., Bamert, R. S., Ruggeri, C., Holleran, J. P., Loganathan, S., Paiardini, A., Charman, S. A., Powell, A. K., Avery, V. M., McGowan, S. & Scammells, P. J., 3 Mar 2016, In : European Journal of Medicinal Chemistry. 110, p. 43-64 22 p.

Research output: Contribution to journalArticleResearchpeer-review

17 Citations (Scopus)

Revisiting the SAR of the antischistosomal aryl hydantoin (Ro 13-3978)

Wang, C., Zhao, Q., Vargas, M., Jones, J. O., White, K., Shackleford, D., Chen, G., Saunders, J., Ng, A., Chiu, F., Dong, Y., Charman, S., Keiser, J. & Vennerstrom, J. L., 8 Dec 2016, In : Journal of Medicinal Chemistry. 59, 23, p. 10705-10718 14 p.

Research output: Contribution to journalArticleResearchpeer-review

12 Citations (Scopus)

Tetrahydro-2-naphthyl and 2-Indanyl triazolopyrimidines targeting Plasmodium falciparum Dihydroorotate Dehydrogenase display potent and selective antimalarial activity

Kokkonda, S., Deng, X., White, K. L., Coteron, J. M., Marco, M., de las Heras, L., White, J., El Mazouni, F., Tomchick, D. R., Manjalanagara, K., Rudra, K. R., Chen, G., Morizzi, J., Ryan, E., Kaminsky, W., Leroy, D., Martínez-Martínez, M. S., Jimenez-Diaz, M. B., Bazaga, S. F., Angulo-Barturen, I. & 6 others, Waterson, D., Burrows, J. N., Matthews, D., Charman, S. A., Phillips, M. A. & Rathod, P. K., 9 Jun 2016, In : Journal of Medicinal Chemistry. 59, 11, p. 5416-5431 16 p.

Research output: Contribution to journalArticleResearchpeer-review

31 Citations (Scopus)
2015

6-arylpyrazine-2-carboxamides: a new core for Trypanosoma brucei inhibitors

Rahmani, R., Ban, K., Jones, A. J., Ferrins, L., Ganame, D., Sykes, M. L., Avery, V. M., White, K. L., Ryan, E., Kaiser, M., Charman, S. A. & Baell, J. B., 2015, In : Journal of Medicinal Chemistry. 58, 17, p. 6753-6765 13 p.

Research output: Contribution to journalArticleResearchpeer-review

13 Citations (Scopus)

A long-duration dihydroorotate dehydrogenase inhibitor (DSM265) for prevention and treatment of malaria

Phillips, M. A., Lotharius, J., Marsh, K., White, J., Dayan, A., White, K. L., Njoroge, J. W., El Mazouni, F., Lao, Y., Kokkonda, S., Tomchick, D. R., Deng, X., Laird, T., Bhatia, S. N., March, S., Ng, C. L., Fidock, D. A., Wittlin, S., Lafuente-Monasterio, M., Gamo Benito, F. J. & 30 others, Sanz Alonso, L. M., Martinez, M. S., Jimenez-Diaz, M. B., Ferrer Bazaga, S., Angulo-Barturen, I., Haselden, J. N., Louttit, J., Cui, Y., Sridhar, A., Zeeman, A-M., Kocken, C., Sauerwein, R. W., Dechering, K., Avery, V. M., Duffy, S., Delves, M., Sinden, R., Ruecker, A., Wickham, K. S., Rochford, R., Gahagen, J., Iyer, L., Riccio, E., Mirsalis, J., Bathhurst, I., Rueckle, T., Ding, X., Campo, B., Leroy, D. & Charman, S. A., 2015, In : Science Translational Medicine. 7, 296, p. 1-12 12 p.

Research output: Contribution to journalArticleResearchpeer-review

125 Citations (Scopus)

A novel multiple-stage antimalarial agent that inhibits protein synthesis

Baragana, B., Hallyburton, I., Lee, M. C. S., Norcross, N. R., Grimaldi, R., Otto, T. D., Proto, W. R., Blagborough, A. M., Meister, S., Wirjanata, G., Ruecker, A., Upton, L. M., Abraham, T. S., Justino de Almeida, M., Pradhan, A., Porzelle, A., Martinez, M. S., Bolscher, J. M., Woodland, A., Norval, S. & 30 others, Zuccotto, F., Thomas, J., Simeons, F., Stojanovski, L., Osuna-Cabello, M., Brock, P. M., Churcher, T. S., Sala, K. A., Zakutansky, S. E., Jimenez-Diaz, M. B., Sanz, L. M., Riley, J., Basak, R., Campbell, M., Avery, V. M., Sauerwein, R. W., Dechering, K. J., Noviyanti, R., Campo, B., Frearson, J. A., Angulo-Barturen, I., Ferrer-Bazaga, S., Gamo, F-J., Wyatt, P. G., Leroy, D., Siegl, P., Delves, M. J., Kyle, D. E., Wittlin, S. & Charman, S. A., 2015, In : Nature. 522, 7556, p. 315-320 6 p.

Research output: Contribution to journalArticleResearchpeer-review

172 Citations (Scopus)

ELQ-300 prodrugs for enhanced delivery and single-dose cure of malaria

Miley, G. P., Pou, S., Winter, R., Nilsen, A., Li, Y., Kelly, J. X., Stickles, A. M., Mather, M. W., Forquer, I. P., Pershing, A. M., White, K., Shackleford, D., Saunders, J., Chen, G., Ting, L-M., Kim, K., Zakharov, L. N., Donini, C., Burrows, J. N., Valdya, A. B. & 2 others, Charman, S. A. & Riscoe, M. K., 2015, In : Antimicrobial Agents and Chemotherapy. 59, 9, p. 5555-5560 6 p.

Research output: Contribution to journalArticleResearchpeer-review

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30 Citations (Scopus)

Enantiomers of nifurtimox do not exhibit stereoselective anti-Trypanosoma cruzi activity, toxicity, or pharmacokinetic properties

Moraes, C. B., White, K. L., Braillard, S., Perez, C., Goo, J., Gaspar, L., Shackleford, D. M., Cordeiro-da-Silva, A., Thompson, R. C. A., Freitas-Junior, L. H., Charman, S. A. & Chatelain, E., 2015, In : Antimicrobial Agents and Chemotherapy. 59, 6, p. 3645-3647 3 p.

Research output: Contribution to journalArticleOtherpeer-review

Open Access

Evidence for the in vitro bioactivation of aminopyrazole derivatives: trapping reactive aminopyrazole intermediates using glutathione ethyl ester in human liver microsomes

Ryan, E., Morrow, B. J., Hemley, C. F., Pinson, J-A., Charman, S. A., Chiu, F. C. K. & Foitzik, R. C., 2015, In : Chemical Research in Toxicology. 28, 9, p. 1747-1752 6 p.

Research output: Contribution to journalArticleResearchpeer-review

2 Citations (Scopus)

Inhibitors of plasmodial serine hydroxymethyltransferase (SHMT): cocrystal structures of pyrazolopyrans with potent blood- and liver-stage activities

Witschel, M. C., Rottmann, M., Schwab, A., Leartsakulpanich, U., Chitnumsub, P., Seet, M., Tonazzi, S., Schwertz, G., Stelzer, F., Mietzner, T., McNamara, C., Thater, F., Freymond, C., Jaruwat, A., Pinthong, C., Riangrungroj, P., Oufir, M., Hamburger, M., Maser, P., Sanz-Alonso, L. M. & 5 others, Charman, S., Wittlin, S., Yuthavong, Y., Chaiyen, P. & Diederich, F., 2015, In : Journal of Medicinal Chemistry. 58, 7, p. 3117-3130 14 p.

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28 Citations (Scopus)

Synthesis and antimalarial evaluation of amide and urea derivatives based on the thiaplakortone A natural product scaffold

Schwartz, B. D., Skinner-Adams, T. S., Andrews, K. T., Coster, M. J., Edstein, M. D., MacKenzie, D., Charman, S. A., Koltun, M., Blundell, S., Campbell, A., Pouwer, R. H., Quinn, R. J., Beattie, K. D., Healy, P. C. & Davis, R. A., 2015, In : Organic and Biomolecular Chemistry. 13, 5, p. 1558-1570 13 p.

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12 Citations (Scopus)

Transformation of poorly water-soluble drugs into lipophilic ionic liquids enhances oral drug exposure from lipid based formulations

Sahbaz, Y., Williams, H. D., Nguyen, T-H., Saunders, J. A., Ford, L., Charman, S. A., Scammells, P. J. & Porter, C. J., 2015, In : Molecular Pharmaceutics. 12, 6, p. 1980 - 1991 12 p.

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64 Citations (Scopus)

Trioxolane-mediated delivery of mefloquine limits brain exposure in a mouse model of malaria

Lauterwasser, E. M. W., Fontaine, S. D., Li, H., Gut, J., Katneni, K., Charman, S. A., Rosenthal, P. J., Bogyo, M. & Renslo, A. R., 2015, In : ACS Medicinal Chemistry Letters. 6, 11, p. 1145-1149 5 p.

Research output: Contribution to journalArticleResearchpeer-review

8 Citations (Scopus)
2014

(+)-SJ733, a clinical candidate for malaria that acts through ATP4 to induce rapid host-mediated clearance of Plasmodium

Jimenez-Diaz, M. B., Ebert, D., Salinas, Y., Pradhan, A., Lehane, A. M., Myrand-Lapierre, M-E., O'Loughlin, K. G., Shackleford, D., Justino de Almeida, M., Carrillo, A., Clark, J. A., Dennis, A. S. M., Diep, J., Deng, X., Duffy, S., Endsley, A. N., Fedewa, G., Guiguemde, W. A., Gomez, M. G., Holbrook, G. & 30 others, Horst, J. A., Kim, C. C., Liu, J., Lee, M. C. S., Matheny, A., Martinez, M. S., Miller, G. E., Rodriguez-Alejandre, A., Sanz, L. M., Sigal, M., Spillman, N. J., Stein, P. D., Wang, Z., Zhu, F., Waterson, D., Knapp, S., Shelat, A. A., Avery, V. M., Fidock, D. A., Gamo, F-J., Charman, S. A., Mirsalis, J. C., Ma, H., Ferrer, S. B., Kirk, K., Angulo-Barturen, I., Kyle, D. E., de Risi, J. L., Floyd, D. M. & Guy, R. K., 2014, In : Proceedings of the National Academy of Sciences of the United States of America. 111, 50, p. e5455 - e5462 8 p.

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110 Citations (Scopus)

2,4-Diaminothienopyrimidines as orally active antimalarial agents

Cabrera, D. G., Le Manach, C., Douelle, F., Younis, Y., Feng, T-S., Paquet, T., Nchinda, A. T., Street, L. J., Taylor, D., de Kock, C., Wiesner, L., Duffy, S., White, K. L., Zabiulla, M. K., Sambandan, Y., Bashyam, S., Waterson, D., Witty, M. J., Charman, S. A., Avery, V. M. & 2 others, Wittlin, S. & Chibale, K., 2014, In : Journal of Medicinal Chemistry. 57, 3, p. 1014 - 1022 9 p.

Research output: Contribution to journalArticleResearchpeer-review

22 Citations (Scopus)

Antitrypanosomal activity of fexinidazole metabolites, potential new drug candidates for Chagas disease

Bahia, M. T., Nascimento, A. F. S., Mazzeti, A. L., Marques, L. F., Goncalves, K. R., Mota, L. W. R., Diniz, L. D. F., Caldas, I. S., Talvani, A., Shackleford, D., Koltun, M., Saunders, J., White, K. L., Scandale, I., Charman, S. A. & Chatelain, E., 2014, In : Antimicrobial Agents and Chemotherapy. 58, 8, p. 4362 - 4370 9 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
31 Citations (Scopus)