Search Results - "CHARMAN, SUSAN A."

Malarial dihydrofolate reductase as a paradigm for drug development against a resistance-compromised target by Yuthavong, Yongyuth, Tarnchompoo, Bongkoch, Vilaivan, Tirayut, Chitnumsub, Penchit, Kamchonwongpaisan, Sumalee, Charman, Susan A., McLennan, Danielle N., White, Karen L., Vivas, Livia, Bongard, Emily, Thongphanchang, Chawanee, Taweechai, Supannee, Vanichtanankul, Jarunee, Rattanajak, Roonglawan, Arwon, Uthai, Fantauzzi, Pascal, Yuvaniyama, Jirundon, Charman, William N., Matthews, David

“…Malarial dihydrofolate reductase (DHFR) is the target of antifolate antimalarial drugs such as pyrimethamine and cycloguanil, the clinical efficacy of which…”
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Fluorine Modulates Species Selectivity in the Triazolopyrimidine Class of Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitors by Deng, Xiaoyi, Kokkonda, Sreekanth, El Mazouni, Farah, White, John, Burrows, Jeremy N, Kaminsky, Werner, Charman, Susan A, Matthews, David, Rathod, Pradipsinh K, Phillips, Margaret A

“…Malaria is one of the most serious global infectious diseases. The pyrimidine biosynthetic enzyme Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH)…”
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Synthetic ozonide drug candidate OZ439 offers new hope for a single-dose cure of uncomplicated malaria by Charman, Susan A., Arbe-Barnes, Sarah, Bathurst, Ian C., Brun, Reto, Campbell, Michael, Charman, William N., Chiu, Francis C. K., Chollet, Jacques, Craft, J. Carl, Creek, Darren J., Dong, Yuxiang, Matile, Hugues, Maurer, Melanie, Morizzi, Julia, Nguyen, Tien, Papastogiannidis, Petros, Scheurer, Christian, Shackleford, David M., Sriraghavan, Kamaraj, Stingelin, Lukas, Tang, Yuanqing, Urwyler, Heinrich, Wang, Xiaofang, White, Karen L., Wittlin, Sergio, Zhou, Lin, Vennerstrom, Jonathan L., Wellems, Thomas E.

“…Ozonide OZ439 is a synthetic peroxide antimalarial drug candidate designed to provide a single-dose oral cure in humans. OZ439 has successfully completed Phase…”
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Endochin-like quinolones are highly efficacious against acute and latent experimental toxoplasmosis by Doggett, J. Stone, Nilsen, Aaron, Forquer, Isaac, Wegmann, Keith W, Jones-Brando, Lorraine, Yolken, Robert H, Bordón, Claudia, Charman, Susan A, Katneni, Kasiram, Schultz, Tracey, Burrows, Jeremy N, Hinrichs, David J, Meunier, Brigitte, Carruthers, Vern B, Riscoe, Michael K

“…Toxoplasma gondii is a widely distributed protozoan pathogen that causes devastating ocular and central nervous system disease. We show that the endochin-like…”
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System-wide biochemical analysis reveals ozonide antimalarials initially act by disrupting Plasmodium falciparum haemoglobin digestion by Giannangelo, Carlo, Siddiqui, Ghizal, De Paoli, Amanda, Anderson, Bethany M, Edgington-Mitchell, Laura E, Charman, Susan A, Creek, Darren J

“…Ozonide antimalarials, OZ277 (arterolane) and OZ439 (artefenomel), are synthetic peroxide-based antimalarials with potent activity against the deadliest…”
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Relationship between Antimalarial Activity and Heme Alkylation for Spiro- and Dispiro-1,2,4-Trioxolane Antimalarials by Creek, Darren J, Charman, William N, Chiu, Francis C K, Prankerd, Richard J, Dong, Yuxiang, Vennerstrom, Jonathan L, Charman, Susan A

“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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Nitroheterocyclic drugs cure experimental Trypanosoma cruzi infections more effectively in the chronic stage than in the acute stage by Francisco, Amanda Fortes, Jayawardhana, Shiromani, Lewis, Michael D., White, Karen L., Shackleford, David M., Chen, Gong, Saunders, Jessica, Osuna-Cabello, Maria, Read, Kevin D., Charman, Susan A., Chatelain, Eric, Kelly, John M.

“…The insect-transmitted protozoan parasite Trypanosoma cruzi is the causative agent of Chagas disease, and infects 5–8 million people in Latin America. Chagas…”
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An in vitro toolbox to accelerate anti-malarial drug discovery and development by Charman, Susan A, Andreu, Alice, Barker, Helena, Blundell, Scott, Campbell, Anna, Campbell, Michael, Chen, Gong, Chiu, Francis C K, Crighton, Elly, Katneni, Kasiram, Morizzi, Julia, Patil, Rahul, Pham, Thao, Ryan, Eileen, Saunders, Jessica, Shackleford, David M, White, Karen L, Almond, Lisa, Dickins, Maurice, Smith, Dennis A, Moehrle, Joerg J, Burrows, Jeremy N, Abla, Nada

“…Modelling and simulation are being increasingly utilized to support the discovery and development of new anti-malarial drugs. These approaches require reliable…”
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Discovery and Structure–Activity Relationships of Quinazolinone-2-carboxamide Derivatives as Novel Orally Efficacious Antimalarials by Laleu, Benoît, Akao, Yuichiro, Ochida, Atsuko, Duffy, Sandra, Lucantoni, Leonardo, Shackleford, David M, Chen, Gong, Katneni, Kasiram, Chiu, Francis C. K, White, Karen L, Chen, Xue, Sturm, Angelika, Dechering, Koen J, Crespo, Benigno, Sanz, Laura M, Wang, Binglin, Wittlin, Sergio, Charman, Susan A, Avery, Vicky M, Cho, Nobuo, Kamaura, Masahiro

“…A phenotypic high-throughput screen allowed discovery of quinazolinone-2-carboxamide derivatives as a novel antimalarial scaffold. Structure–activity…”
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Discovery, Synthesis, and Optimization of Antimalarial 4(1H)‑Quinolone-3-Diarylethers by Nilsen, Aaron, Miley, Galen P, Forquer, Isaac P, Mather, Michael W, Katneni, Kasiram, Li, Yuexin, Pou, Sovitj, Pershing, April M, Stickles, Allison M, Ryan, Eileen, Kelly, Jane Xu, Doggett, J. Stone, White, Karen L, Hinrichs, David J, Winter, Rolf W, Charman, Susan A, Zakharov, Lev N, Bathurst, Ian, Burrows, Jeremy N, Vaidya, Akhil B, Riscoe, Michael K

“…The historical antimalarial compound endochin served as a structural lead for optimization. Endochin-like quinolones (ELQ) were prepared by a novel chemical…”
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Structure–Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439) by Dong, Yuxiang, Wang, Xiaofang, Kamaraj, Sriraghavan, Bulbule, Vivek J, Chiu, Francis C. K, Chollet, Jacques, Dhanasekaran, Manickam, Hein, Christopher D, Papastogiannidis, Petros, Morizzi, Julia, Shackleford, David M, Barker, Helena, Ryan, Eileen, Scheurer, Christian, Tang, Yuanqing, Zhao, Qingjie, Zhou, Lin, White, Karen L, Urwyler, Heinrich, Charman, William N, Matile, Hugues, Wittlin, Sergio, Charman, Susan A, Vennerstrom, Jonathan L

“…Building on insights gained from the discovery of the antimalarial ozonide arterolane (OZ277), we now describe the structure–activity relationship (SAR) of the…”
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Discovery and Structure–Activity Relationships of Pyrrolone Antimalarials by Murugesan, Dinakaran, Mital, Alka, Kaiser, Marcel, Shackleford, David M, Morizzi, Julia, Katneni, Kasiram, Campbell, Michael, Hudson, Alan, Charman, Susan A, Yeates, Clive, Gilbert, Ian H

“…In the pursuit of new antimalarial leads, a phenotypic screening of various commercially sourced compound libraries was undertaken by the World Health…”
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3,5-Diaryl-2-aminopyridines as a Novel Class of Orally Active Antimalarials Demonstrating Single Dose Cure in Mice and Clinical Candidate Potential by Younis, Yassir, Douelle, Frederic, Feng, Tzu-Shean, Cabrera, Diego González, Manach, Claire Le, Nchinda, Aloysius T, Duffy, Sandra, White, Karen L, Shackleford, David M, Morizzi, Julia, Mannila, Janne, Katneni, Kasiram, Bhamidipati, Ravi, Zabiulla, K. Mohammed, Joseph, Jayan T, Bashyam, Sridevi, Waterson, David, Witty, Michael J, Hardick, David, Wittlin, Sergio, Avery, Vicky, Charman, Susan A, Chibale, Kelly

“…A novel class of orally active antimalarial 3,5-diaryl-2-aminopyridines has been identified from phenotypic whole cell high-throughput screening of a…”
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Sansanmycin natural product analogues as potent and selective anti-mycobacterials that inhibit lipid I biosynthesis by Tran, Anh T., Watson, Emma E., Pujari, Venugopal, Conroy, Trent, Dowman, Luke J., Giltrap, Andrew M., Pang, Angel, Wong, Weng Ruh, Linington, Roger G., Mahapatra, Sebabrata, Saunders, Jessica, Charman, Susan A., West, Nicholas P., Bugg, Timothy D. H., Tod, Julie, Dowson, Christopher G., Roper, David I., Crick, Dean C., Britton, Warwick J., Payne, Richard J.

“…Tuberculosis (TB) is responsible for enormous global morbidity and mortality, and current treatment regimens rely on the use of drugs that have been in use for…”
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Selecting an anti-malarial clinical candidate from two potent dihydroisoquinolones by Chen, Yizhe, Zhu, Fangyi, Hammill, Jared, Holbrook, Gloria, Yang, Lei, Freeman, Burgess, White, Karen L, Shackleford, David M, O'Loughlin, Kathleen G, Charman, Susan A, Mirsalis, Jon C, Guy, R Kiplin

“…The ongoing global malaria eradication campaign requires development of potent, safe, and cost-effective drugs lacking cross-resistance with existing…”
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Bioisosteric Transformations and Permutations in the Triazolopyrimidine Scaffold To Identify the Minimum Pharmacophore Required for Inhibitory Activity against Plasmodium falciparum Dihydroorotate Dehydrogenase by Marwaha, Alka, White, John, El_Mazouni, Farah, Creason, Sharon A, Kokkonda, Sreekanth, Buckner, Frederick S, Charman, Susan A, Phillips, Margaret A, Rathod, Pradipsinh K

“…Plasmodium falciparum causes approximately 1 million deaths annually. However, increasing resistance imposes a continuous threat to existing drug therapies. We…”
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Intestinal Lymph Flow, and Lipid and Drug Transport Scale Allometrically From Pre-clinical Species to Humans by Trevaskis, Natalie L., Lee, Given, Escott, Alistair, Phang, Kian Liun, Hong, Jiwon, Cao, Enyuan, Katneni, Kasiram, Charman, Susan A., Han, Sifei, Charman, William N., Phillips, Anthony R. J., Windsor, John A., Porter, Christopher J. H.

“…The intestinal lymphatic system transports fluid, immune cells, dietary lipids, and highly lipophilic drugs from the intestine to the systemic circulation…”
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On-target, dual aminopeptidase inhibition provides cross-species antimalarial activity by Edgar, Rebecca C S, Malcolm, Tess R, Siddiqui, Ghizal, Giannangelo, Carlo, Counihan, Natalie A, Challis, Matthew, Duffy, Sandra, Chowdhury, Mrittika, Marfurt, Jutta, Dans, Madeline, Wirjanata, Grennady, Noviyanti, Rintis, Daware, Kajal, Suraweera, Chathura D, Price, Ric N, Wittlin, Sergio, Avery, Vicky M, Drinkwater, Nyssa, Charman, Susan A, Creek, Darren J, de Koning-Ward, Tania F, Scammells, Peter J, McGowan, Sheena

“…To combat the global burden of malaria, development of new drugs to replace or complement current therapies is urgently required. Here, we show that the…”
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Hit-to-Lead Optimization of a Novel Class of Potent, Broad-Spectrum Trypanosomacides by Russell, Stephanie, Rahmani, Raphaël, Jones, Amy J, Newson, Harriet L, Neilde, Kevin, Cotillo, Ignacio, Rahmani Khajouei, Marzieh, Ferrins, Lori, Qureishi, Sana, Nguyen, Nghi, Martinez-Martinez, Maria S, Weaver, Donald F, Kaiser, Marcel, Riley, Jennifer, Thomas, John, De Rycker, Manu, Read, Kevin D, Flematti, Gavin R, Ryan, Eileen, Tanghe, Scott, Rodriguez, Ana, Charman, Susan A, Kessler, Albane, Avery, Vicky M, Baell, Jonathan B, Piggott, Matthew J

“…The parasitic trypanosomes Trypanosoma brucei and T. cruzi are responsible for significant human suffering in the form of human African trypanosomiasis (HAT)…”
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Antimalarial Activity of Pyrroloiminoquinones from the Australian Marine Sponge Zyzzya sp by Davis, Rohan A, Buchanan, Malcolm S, Duffy, Sandra, Avery, Vicky M, Charman, Susan A, Charman, William N, White, Karen L, Shackleford, David M, Edstein, Michael D, Andrews, Katherine T, Camp, David, Quinn, Ronald J

“…A new bispyrroloiminoquinone alkaloid, tsitsikammamine C (1), displayed potent in vitro antimalarial activity with IC50 values of 13 and 18 nM against…”
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