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Research Output 1991 2019

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2019

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 othersSleebs, B. E., 1 Mar 2019, In : Antimicrobial Agents and Chemotherapy. 63, 3, 15 p., e01804-18.

Research output: Contribution to journalArticleResearchpeer-review

2018

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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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

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

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

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 othersCharman, S. A., 26 Apr 2017, In : Science Translational Medicine. 9, 387, 14 p., eaad9735.

Research output: Contribution to journalArticleResearchpeer-review

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 othersDiederich, F., 22 Jun 2017, In : Journal of Medicinal Chemistry. 60, 12, p. 4840-4860 21 p.

Research output: Contribution to journalArticleResearchpeer-review

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 othersRyan, 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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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
File

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

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

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 othersMatile, 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

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 othersHuggins, 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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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 othersCharman, S., 9 Dec 2016, In : ACS Infectious Diseases. 2, 12, p. 945-957 13 p.

Research output: Contribution to journalArticleResearchpeer-review

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

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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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 othersRodriguez, 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

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

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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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 othersRyan, 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

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

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

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 othersWaterson, 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

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

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 othersSanz 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

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 othersZuccotto, 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

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 othersCharman, S. A. & Riscoe, M. K., 2015, In : Antimicrobial Agents and Chemotherapy. 59, 9, p. 5555-5560 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access

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

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 othersCharman, S., Wittlin, S., Yuthavong, Y., Chaiyen, P. & Diederich, F., 2015, In : Journal of Medicinal Chemistry. 58, 7, p. 3117-3130 14 p.

Research output: Contribution to journalArticleResearchpeer-review

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.

Research output: Contribution to journalArticleResearchpeer-review

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.

Research output: Contribution to journalArticleResearchpeer-review

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 : A C S Medicinal Chemistry Letters. 6, 11, p. 1145-1149 5 p.

Research output: Contribution to journalArticleResearchpeer-review

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 othersHorst, 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. 111, 50, p. e5455 - e5462 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access

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 othersWittlin, S. & Chibale, K., 2014, In : Journal of Medicinal Chemistry. 57, 3, p. 1014 - 1022 9 p.

Research output: Contribution to journalArticleResearchpeer-review

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

Development of diaminoquinazoline histone lysine methyltransferase inhibitors as potent blood-stage antimalarial compounds

Sundriyal, S., Malmquist, N. A., Caron, J., Blundell, S., Liu, F., Chen, X., Srimongkolpithak, N., Jin, JI., Charman, S. A., Scherf, A. & Fuchter, M. J., 2014, In : ChemMedChem. 9, 10, p. 2360 - 2373 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Discovery, synthesis, and optimization of antimalarial 4(1H)-quinolone-3-diarylethers

Nilsen, A., Miley, G. P., Forquer, I. P., Mather, M. W., Katneni, K., Li, Y., Pou, S., Pershing, A. M., Stickles, A. M., Ryan, E., Kelly, J. X., Doggett, J. S., White, K. L., Hinrichs, D. J., Winter, R. W., Charman, S. A., Zakharov, L. N., Bathurst, I. C., Burrows, J., Vaidya, A. B. & 1 othersRiscoe, M. K., 2014, In : Journal of Medicinal Chemistry. 57, 9, p. 3818 - 3834 17 p.

Research output: Contribution to journalArticleResearchpeer-review

Fluorine modulates species selectivity in the triazolopyrimidine class of Plasmodium falciparum dihydroorotate dehydrogenase inhibitors

Deng, X., Kokkonda, S., El Mazouni, F., White, J., Burrows, J., Kaminsky, W., Charman, S. A., Matthews, D., Rathod, P. K. & Phillips, M. A., 2014, In : Journal of Medicinal Chemistry. 57, 12, p. 5381 - 5394 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a SoftFocus kinase library: Part 1

Le Manach, C., Cabrera, D. G., Douelle, F., Nchinda, A. T., Younis, Y., Taylor, D., Wiesner, L., White, K. L., Ryan, E., March, C., Duffy, S., Avery, V. M., Waterson, D., Witty, M. J., Wittlin, S., Charman, S. A., Street, L. J. & Chibale, K., 2014, In : Journal of Medicinal Chemistry. 57, 6, p. 2789 - 2798 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Orally bioavailable 6-chloro-7-methoxy-4(1H)-quinolones efficacious against multiple stages of Plasmodium

Cross, M., Flanigan, D. L., Monastyrskyi, A., LaCrue, A. N., Saenz, F. E., Maignan, J. R., Mutka, T. S., White, K. L., Shackleford, D., Bathurst, I. C., Fronczek, F. R., Wojtas, L., Guida, W. C., Charman, S. A., Burrows, J., Kyle, D. E. & Manetsch, R., 2014, In : Journal of Medicinal Chemistry. 57, 21, p. 8860 - 8879 20 p.

Research output: Contribution to journalArticleResearchpeer-review

Pyrazoleamide compounds are potent antimalarials that target Na+ homeostasis in intraerythrocytic Plasmodium falciparum

Vaidya, A. B., Morrisey, J. M., Zhang, Z., Das, S., Daly, T. M., Otto, T. D., Spillman, N. J., Wyvratt, M., Siegl, P., Marfurt, J., Wirjanata, G., Sebayang, B. F., Price, R. N., Chatterjee, A., Nagle, A. S., Stasiak, M., Charman, S. A., Angulo-Barturen, I., Ferrer, S. B., Jimenez-Diaz, M. B. & 11 othersMartinez, M. S., Gamo-Benito, F. J., Avery, V. M., Ruecker, A., Delves, M. J., Kirk, K., Berriman, M., Kortagere, S., Burrows, J., Fan, E. & Bergman, L. W., 2014, In : Nature Communications. 5, 5521, p. 1 - 10 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access

Pyridyl benzamides as a novel class of potent inhibitors for the kinetoplastid Trypanosoma brucei

Ferrins, L., Gazdik, M., Rahmani, R. S., Varghese, S., Sykes, M. L., Jones, A. J., Avery, V. M., White, K. L., Ryan, E., Charman, S. A., Kaiser, M., Bergstrom, C. A. S. & Baell, J. B., 2014, In : Journal of Medicinal Chemistry. 57, 15, p. 6393 - 6402 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Total synthesis of thiaplakortone A: Derivatives as metabolically stable leads for the treatment of malaria

Pouwer, R. H., Deydier, S. M., Le, P. V., Schwartz, B. D., Franken, N. C., Davis, R. A., Coster, M., Charman, S. A., Edstein, M. D., Skinner-Adams, T. S., Andrews, K. T., Jenkins, I. D. & Quinn, R. J., 2014, In : A C S Medicinal Chemistry Letters. 5, 2, p. 178 - 182 5 p.

Research output: Contribution to journalArticleResearchpeer-review

2013

3-(Oxazolo[4,5-b]pyridin-2-yl)anilides as a novel class of potent inhibitors for the kinetoplastid Trypanosoma brucei, the causative agent for human African trypanosomiasis

Ferrins, L., Rahmani, R. S., Sykes, M. L., Jones, A. J., Avery, V. M., Teston, E., Almohaywi, B., Yin, J., Smith, J., Chris, H., White, K. L., Ryan, E., Campbell, M., Charman, S. A., Kaiser, M. & Baell, J. B., 2013, In : European Journal of Medicinal Chemistry. 66, p. 450 - 465 16 p.

Research output: Contribution to journalArticleResearchpeer-review

A prodrug approach toward cancer-related carbonic anhydrase inhibition

Carroux, C. J., Rankin, G. M., Moeker, J., Bornaghi, L. F., Katneni, K., Morizzi, J., Charman, S. A., Vullo, D., Supuran, C. T. & Poulsen, S-A., 2013, In : Journal of Medicinal Chemistry. 56, 23, p. 9623 - 9634 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres

Wang, X., Dong, Y., Wittlin, S., Charman, S. A., Chiu, F. C. K., Chollet, J., Katneni, K., Mannila, J. M., Morizzi, J., Ryan, E., Scheurer, C., Steuten, J. A., Santo Tomas, J., Snyder, C. & Vennerstrom, J., 2013, In : Journal of Medicinal Chemistry. 56, 6, p. 2547 - 2555 9 p.

Research output: Contribution to journalArticleResearchpeer-review

Complexes of Trypanosoma cruzi sterol 14a-demethylase (CYP51) with two pyridine-based drug candidates for Chagas disease: Structural basis for pathogen selectivity

Hargrove, T. Y., Wawrzak, Z., Alexander, P. W., Chaplin, J. H., Keenan, M., Charman, S. A., Perez, C., Waterman, M., Chatelain, E. & Lepesheva, G. I., 2013, In : Journal of Biological Chemistry. 288, 44, p. 31602 - 31615 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Design, structure-activity relationship and in vivo efficacy of piperazine analogues of fenarimol as inhibitors of Trypanosoma cruzi

Keenan, M., Alexander, P. W., Diao, H., Best, W. M., Khong, A., Kerfoot, M., Thompson, R. C. A., White, K. L., Shackleford, D., Ryan, E., Gregg, A. D., Charman, S. A., von Geldern, T. W., Scandale, I. & Chatelain, E., 2013, In : Bioorganic & Medicinal Chemistry. 21, 7, p. 1756 - 1763 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Discovery and structure-activity relationships of pyrrolone antimalarials

Murugesan, D., Mital, A., Kaiser, M., Shackleford, D., Morizzi, J., Katneni, K., Campbell, M., Hudson, A., Charman, S. A., Yeates, C. & Gilbert, I. H., 2013, In : Journal of Medicinal Chemistry. 56, 7, p. 2975 - 2990 16 p.

Research output: Contribution to journalArticleResearchpeer-review