Structure-Guided Lead Optimization of Triazolopyrimidine-Ring Substituents Identifies Potent Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitors with Clinical Candidate Potential
Coteron, Jose M, Marco, María, Esquivias, Jorge, Deng, Xiaoyi, White, Karen L, White, John, Koltun, Maria, El Mazouni, Farah, Kokkonda, Sreekanth, Katneni, Kasiram, Bhamidipati, Ravi, Shackleford, David M, Angulo-Barturen, Iñigo, Ferrer, Santiago B, Jiménez-Díaz, María Belén, Gamo, Francisco-Javier, Goldsmith, Elizabeth J, Charman, William N, Bathurst, Ian, Floyd, David, Matthews, David, Burrows, Jeremy N, Rathod, Pradipsinh K, Charman, Susan A, Phillips, Margaret A
Published in Journal of medicinal chemistry (11.08.2011)
Published in Journal of medicinal chemistry (11.08.2011)
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A novel class of fast‐acting antimalarial agents: Substituted 15‐membered azalides
Peric, Mihaela, Pešić, Dijana, Alihodžić, Sulejman, Fajdetić, Andrea, Herreros, Esperanza, Gamo, Francisco Javier, Angulo‐Barturen, Iñigo, Jiménez‐Díaz, María Belén, Ferrer‐Bazaga, Santiago, Martínez, María S., Gargallo‐Viola, Domingo, Mathis, Amanda, Kessler, Albane, Banjanac, Mihailo, Padovan, Jasna, Bencetić Mihaljević, Vlatka, Munic Kos, Vesna, Bukvić, Mirjana, Eraković Haber, Vesna, Spaventi, Radan
Published in British journal of pharmacology (01.01.2021)
Published in British journal of pharmacology (01.01.2021)
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A Novel Pyrazolopyridine with in Vivo Activity in Plasmodium berghei- and Plasmodium falciparum -Infected Mouse Models from Structure–Activity Relationship Studies around the Core of Recently Identified Antimalarial Imidazopyridazines
Le Manach, Claire, Paquet, Tanya, Brunschwig, Christel, Njoroge, Mathew, Han, Ze, Gonzàlez Cabrera, Diego, Bashyam, Sridevi, Dhinakaran, Rajkumar, Taylor, Dale, Reader, Janette, Botha, Mariette, Churchyard, Alisje, Lauterbach, Sonja, Coetzer, Theresa L, Birkholtz, Lyn-Marie, Meister, Stephan, Winzeler, Elizabeth A, Waterson, David, Witty, Michael J, Wittlin, Sergio, Jiménez-Díaz, María-Belén, Santos Martínez, María, Ferrer, Santiago, Angulo-Barturen, Iñigo, Street, Leslie J, Chibale, Kelly
Published in Journal of medicinal chemistry (12.11.2015)
Published in Journal of medicinal chemistry (12.11.2015)
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Using Cryopreserved Plasmodium falciparum Sporozoites in a Humanized Mouse Model to Study Early Malaria Infection Processes and Test Prophylactic Treatments
Jiménez-Díaz, María-Belén, Möhrle, Jörg J, Angulo-Barturen, Iñigo, Demarta-Gatsi, Claudia
Published in Microorganisms (Basel) (31.08.2023)
Published in Microorganisms (Basel) (31.08.2023)
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Feasibility of Flow Cytometry for Measurements of Plasmodium falciparum Parasite Burden in Studies in Areas of Malaria Endemicity by Use of Bidimensional Assessment of YOYO-1 and Autofluorescence
CAMPO, Joseph J, APONTE, John J, NHABOMBA, Augusto J, SACARLAL, Jahit, ANGULO-BARTUREN, Iñigo, JIMENEZ-DIAZ, Maria Belén, ALONSO, Pedro L, DOBANO, Carlota
Published in Journal of Clinical Microbiology (01.03.2011)
Published in Journal of Clinical Microbiology (01.03.2011)
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Macrocyclic Peptidomimetic Plasmepsin X Inhibitors with Potent In Vitro and In Vivo Antimalarial Activity
Kovada, Vadims, Withers-Martinez, Chrislaine, Bobrovs, Raitis, Ce̅rule, Hele̅na, Liepins, Edgars, Grinberga, Solveiga, Hackett, Fiona, Collins, Christine R., Kreicberga, Agrita, Jiménez-Díaz, María Belén, Angulo-Barturen, Iñigo, Rasina, Dace, Suna, Edgars, Jaudzems, Kristaps, Blackman, Michael J., Jirgensons, Aigars
Published in Journal of medicinal chemistry (10.08.2023)
Published in Journal of medicinal chemistry (10.08.2023)
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Predicting Optimal Antimalarial Drug Combinations from a Standardized Plasmodium falciparum Humanized Mouse Model
Demarta-Gatsi, Claudia, Andenmatten, Nicole, Jiménez-Díaz, María-Belén, Gobeau, Nathalie, Cherkaoui-Rabti, Mohammed H, Fuchs, Aline, Díaz, Pablo, Berja, Sandra, Sánchez, Rebeca, Gómez, Hazel, Ruiz, Estíbaliz, Sainz, Paula, Salazar, Eider, Gil-Merino, Rodrigo, Mendoza, Luis Manuel, Eguizabal, Cristina, Leroy, Didier, Moehrle, Joerg J, Tornesi, Belen, Angulo-Barturen, Iñigo
Published in Antimicrobial agents and chemotherapy (15.06.2023)
Published in Antimicrobial agents and chemotherapy (15.06.2023)
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Discovery and Preclinical Pharmacology of INE963, a Potent and Fast-Acting Blood-Stage Antimalarial with a High Barrier to Resistance and Potential for Single-Dose Cures in Uncomplicated Malaria
Taft, Benjamin R, Yokokawa, Fumiaki, Kirrane, Tom, Mata, Anne-Catherine, Huang, Richard, Blaquiere, Nicole, Waldron, Grace, Zou, Bin, Simon, Oliver, Vankadara, Subramanyam, Chan, Wai Ling, Ding, Mei, Sim, Sandra, Straimer, Judith, Guiguemde, Armand, Lakshminarayana, Suresh B, Jain, Jay Prakash, Bodenreider, Christophe, Thompson, Christopher, Lanshoeft, Christian, Shu, Wei, Fang, Eric, Qumber, Jafri, Chan, Katherine, Pei, Luying, Chen, Yen-Liang, Schulz, Hanna, Lim, Jessie, Abas, Siti Nurdiana, Ang, Xiaoman, Liu, Yugang, Angulo-Barturen, Iñigo, Jiménez-Díaz, María Belén, Gamo, Francisco Javier, Crespo-Fernandez, Benigno, Rosenthal, Philip J, Cooper, Roland A, Tumwebaze, Patrick, Aguiar, Anna Caroline Campos, Campo, Brice, Campbell, Simon, Wagner, Jürgen, Diagana, Thierry T, Sarko, Christopher
Published in Journal of medicinal chemistry (10.03.2022)
Published in Journal of medicinal chemistry (10.03.2022)
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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, Claire, Nchinda, Aloysius T, Paquet, Tanya, Gonzàlez Cabrera, Diego, Younis, Yassir, Han, Ze, Bashyam, Sridevi, Zabiulla, Mohammed, Taylor, Dale, Lawrence, Nina, White, Karen L, Charman, Susan A, Waterson, David, Witty, Michael J, Wittlin, Sergio, Botha, Mariëtte E, Nondaba, Sindisiswe H, Reader, Janette, Birkholtz, Lyn-Marie, Jiménez-Díaz, María Belén, Martínez, María Santos, Ferrer, Santiago, Angulo-Barturen, Iñigo, Meister, Stephan, Antonova-Koch, Yevgeniya, Winzeler, Elizabeth A, Street, Leslie J, Chibale, Kelly
Published in Journal of medicinal chemistry (10.11.2016)
Published in Journal of medicinal chemistry (10.11.2016)
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A murine model of falciparum-malaria by in vivo selection of competent strains in non-myelodepleted mice engrafted with human erythrocytes
Angulo-Barturen, Iñigo, Jiménez-Díaz, María Belén, Mulet, Teresa, Rullas, Joaquín, Herreros, Esperanza, Ferrer, Santiago, Jiménez, Elena, Mendoza, Alfonso, Regadera, Javier, Rosenthal, Philip J, Bathurst, Ian, Pompliano, David L, Gómez de las Heras, Federico, Gargallo-Viola, Domingo
Published in PloS one (21.05.2008)
Published in PloS one (21.05.2008)
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N‑Aryl-2-aminobenzimidazoles: Novel, Efficacious, Antimalarial Lead Compounds
Ramachandran, Sreekanth, Hameed P, Shahul, Srivastava, Abhishek, Shanbhag, Gajanan, Morayya, Sapna, Rautela, Nikhil, Awasthy, Disha, Kavanagh, Stefan, Bharath, Sowmya, Reddy, Jitendar, Panduga, Vijender, Prabhakar, K. R, Saralaya, Ramanatha, Nanduri, Robert, Raichurkar, Anandkumar, Menasinakai, Sreenivasaiah, Achar, Vijayashree, Jiménez-Díaz, María Belén, Martínez, María Santos, Angulo-Barturen, Iñigo, Ferrer, Santiago, Sanz, Laura María, Gamo, Francisco Javier, Duffy, Sandra, Avery, Vicky M, Waterson, David, Lee, Marcus C. S, Coburn-Flynn, Olivia, Fidock, David A, Iyer, Pravin S, Narayanan, Shridhar, Hosagrahara, Vinayak, Sambandamurthy, Vasan K
Published in Journal of medicinal chemistry (14.08.2014)
Published in Journal of medicinal chemistry (14.08.2014)
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Improvement of detection specificity of Plasmodium‐infected murine erythrocytes by flow cytometry using autofluorescence and YOYO‐1
Jiménez‐Díaz, María Belén, Rullas, Joaquín, Mulet, Teresa, Fernández, Laura, Bravo, Carmen, Gargallo‐Viola, Domingo, Angulo‐Barturen, Iñigo
Published in Cytometry. Part A (01.09.2005)
Published in Cytometry. Part A (01.09.2005)
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Carbamoyl Triazoles, Known Serine Protease Inhibitors, Are a Potent New Class of Antimalarials
McConville, Matthew, Fernández, Jorge, Angulo-Barturen, Íñigo, Bahamontes-Rosa, Noemi, Ballell-Pages, Lluis, Castañeda, Pablo, de Cózar, Cristina, Crespo, Benigno, Guijarro, Laura, Jiménez-Díaz, María Belén, Martínez-Martínez, Maria S, de Mercado, Jaime, Santos-Villarejo, Ángel, Sanz, Laura M, Frigerio, Micol, Washbourn, Gina, Ward, Stephen A, Nixon, Gemma L, Biagini, Giancarlo A, Berry, Neil G, Blackman, Michael J, Calderón, Félix, O’Neill, Paul M
Published in Journal of medicinal chemistry (27.08.2015)
Published in Journal of medicinal chemistry (27.08.2015)
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Improved Murine Model of Malaria Using Plasmodium falciparum Competent Strains and Non-Myelodepleted NOD-scid IL2Rγnull Mice Engrafted with Human Erythrocytes
Jiménez-Díaz, María Belén, Mulet, Teresa, Viera, Sara, Gómez, Vanessa, Garuti, Helen, Ibáñez, Javier, Alvarez-Doval, Angela, Shultz, Leonard D., Martínez, Antonio, Gargallo-Viola, Domingo, Angulo-Barturen, Iñigo
Published in Antimicrobial Agents and Chemotherapy (01.10.2009)
Published in Antimicrobial Agents and Chemotherapy (01.10.2009)
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Long-Lasting and Fast-Acting in Vivo Efficacious Antiplasmodial Azepanylcarbazole Amino Alcohol
Abla, Nada, Bashyam, Sridevi, Charman, Susan A, Greco, Béatrice, Hewitt, Philip, Jiménez-Díaz, Maria Belén, Katneni, Kasiram, Kubas, Holger, Picard, Didier, Sambandan, Yuvaraj, Sanz, Laura, Smith, Dennis, Wang, Tai, Willis, Paul, Wittlin, Sergio, Spangenberg, Thomas
Published in ACS medicinal chemistry letters (14.12.2017)
Published in ACS medicinal chemistry letters (14.12.2017)
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Quantitative measurement of Plasmodium‐infected erythrocytes in murine models of malaria by flow cytometry using bidimensional assessment of SYTO‐16 fluorescence
Jiménez‐Díaz, María Belén, Mulet, Teresa, Gómez, Vanesa, Viera, Sara, Alvarez, Angela, Garuti, Helena, Vázquez, Yolanda, Fernández, Alejandra, Ibáñez, Javier, Jiménez, Magdalena, Gargallo‐Viola, Domingo, Angulo‐Barturen, Iñigo
Published in Cytometry. Part A (01.03.2009)
Published in Cytometry. Part A (01.03.2009)
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A Divergent SAR Study Allows Optimization of a Potent 5-HT2c Inhibitor to a Promising Antimalarial Scaffold
Calderón, Félix, Vidal-Mas, Jaume, Burrows, Jeremy, de la Rosa, Juan Carlos, Jiménez-Díaz, María Belén, Mulet, Teresa, Prats, Sara, Solana, Jorge, Witty, Michael, Gamo, Francisco Javier, Fernández, Esther
Published in ACS medicinal chemistry letters (10.05.2012)
Published in ACS medicinal chemistry letters (10.05.2012)
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Potent Antimalarials with Development Potential Identified by Structure-Guided Computational Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series
Palmer, Michael J, Deng, Xiaoyi, Watts, Shawn, Krilov, Goran, Gerasyuto, Aleksey, Kokkonda, Sreekanth, El Mazouni, Farah, White, John, White, Karen L, Striepen, Josefine, Bath, Jade, Schindler, Kyra A, Yeo, Tomas, Shackleford, David M, Mok, Sachel, Deni, Ioanna, Lawong, Aloysus, Huang, Ann, Chen, Gong, Wang, Wen, Jayaseelan, Jaya, Katneni, Kasiram, Patil, Rahul, Saunders, Jessica, Shahi, Shatrughan P, Chittimalla, Rajesh, Angulo-Barturen, Iñigo, Jiménez-Díaz, María Belén, Wittlin, Sergio, Tumwebaze, Patrick K, Rosenthal, Philip J, Cooper, Roland A, Aguiar, Anna Caroline Campos, Guido, Rafael V. C, Pereira, Dhelio B, Mittal, Nimisha, Winzeler, Elizabeth A, Tomchick, Diana R, Laleu, Benoît, Burrows, Jeremy N, Rathod, Pradipsinh K, Fidock, David A, Charman, Susan A, Phillips, Margaret A
Published in Journal of medicinal chemistry (13.05.2021)
Published in Journal of medicinal chemistry (13.05.2021)
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Discovery and Characterization of Potent, Efficacious, Orally Available Antimalarial Plasmepsin X Inhibitors and Preclinical Safety Assessment of UCB7362
Lowe, Martin A., Cardenas, Alvaro, Valentin, Jean-Pierre, Zhu, Zhaoning, Abendroth, Jan, Castro, Jose L., Class, Reiner, Delaunois, Annie, Fleurance, Renaud, Gerets, Helga, Gryshkova, Vitalina, King, Lloyd, Lorimer, Donald D., MacCoss, Malcolm, Rowley, Julian H., Rosseels, Marie-Luce, Royer, Leandro, Taylor, Richard D., Wong, Melanie, Zaccheo, Oliver, Chavan, Vishal P., Ghule, Gokul A., Tapkir, Bapusaheb K., Burrows, Jeremy N., Duffey, Maëlle, Rottmann, Matthias, Wittlin, Sergio, Angulo-Barturen, Iñigo, Jiménez-Díaz, María Belén, Striepen, Josefine, Fairhurst, Kate J., Yeo, Tomas, Fidock, David A., Cowman, Alan F., Favuzza, Paola, Crespo-Fernandez, Benigno, Gamo, Francisco Javier, Goldberg, Daniel E., Soldati-Favre, Dominique, Laleu, Benoît, de Haro, Teresa
Published in Journal of medicinal chemistry (27.10.2022)
Published in Journal of medicinal chemistry (27.10.2022)
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UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria
Brunschwig, Christel, Lawrence, Nina, Taylor, Dale, Abay, Efrem, Njoroge, Mathew, Basarab, Gregory S, Le Manach, Claire, Paquet, Tanya, Cabrera, Diego Gonzàlez, Nchinda, Aloysius T, de Kock, Carmen, Wiesner, Lubbe, Denti, Paolo, Waterson, David, Blasco, Benjamin, Leroy, Didier, Witty, Michael J, Donini, Cristina, Duffy, James, Wittlin, Sergio, White, Karen L, Charman, Susan A, Jiménez-Díaz, Maria Belén, Angulo-Barturen, Iñigo, Herreros, Esperanza, Gamo, Francisco Javier, Rochford, Rosemary, Mancama, Dalu, Coetzer, Theresa L, van der Watt, Mariëtte E, Reader, Janette, Birkholtz, Lyn-Marie, Marsh, Kennan C, Solapure, Suresh M, Burke, John E, McPhail, Jacob A, Vanaerschot, Manu, Fidock, David A, Fish, Paul V, Siegl, Peter, Smith, Dennis A, Wirjanata, Grennady, Noviyanti, Rintis, Price, Ric N, Marfurt, Jutta, Silue, Kigbafori D, Street, Leslie J, Chibale, Kelly
Published in Antimicrobial agents and chemotherapy (01.09.2018)
Published in Antimicrobial agents and chemotherapy (01.09.2018)
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