Optimization of pyrazolopyridine 4-carboxamides with potent antimalarial activity for which resistance is associated with the P. falciparum transporter ABCI3

Authors: Calic, Petar P.S., Ashton, Trent D., Mansouri, Mahta, Loi, Katie, Jarman, Kate E., Qiu, Deyun, Lehane, Adele M., Roy, Sayantan, Rao, Gunturu P., Maity, Bikash, Wittlin, Sergio, Crespo, Benigno, Gamo, Franciso-Javier, Deni, Ioanna, Fidock, David A., Chowdury, Mrittika, de Koning-Ward, Tania F., Cowman, Alan F., Jackson, Paul F., Baud, Delphine, Brand, Stephen, Laleu, Benoît, Sleebs, Brad E.

Source: In European Journal of Medicinal Chemistry 5 October 2024 276

Exploring the unexplored chemical space: Rational identification of new Tafenoquine analogs with antimalarial properties

Authors: Manen-Freixa, Leticia, Moliner-Cubel, Sonia, Gamo, Francisco-Javier, Crespo, Benigno, Borrell, José I., Teixidó, Jordi, Estrada-Tejedor, Roger

Source: In Bioorganic Chemistry July 2024 148

A potent and selective reaction hijacking inhibitor of Plasmodium falciparum tyrosine tRNA synthetase exhibits single dose oral efficacy in vivo.

Authors: Xie, Stanley C.^1,2, Tai, Chia-Wei¹, Morton, Craig J.³, Ma, Liting⁴, Huang, Shih-Chung⁴, Wittlin, Sergio^5,6, Du, Yawei¹, Hu, Yongbo⁴, Dogovski, Con¹, Salimimarand, Mina⁷, Griffin, Robert⁴, England, Dylan⁴, de la Cruz, Elisa⁴, Deni, Ioanna^8,9, Yeo, Tomas^8,9, Burkhard, Anna Y.^8,9, Striepen, Josefine^8,9, Schindler, Kyra A.^8,9, Crespo, Benigno¹⁰, Gamo, Francisco J.¹⁰

Source: PLoS Pathogens; 12/9/2024, Vol. 20 Issue 12, p1-28, 28p

High-Content Phenotypic Screen of a Focused TCAMS Drug Library Identifies Novel Disruptors of the Malaria Parasite Calcium Dynamics

Authors: Chia, Wanni, Gomez-Lorenzo, Maria G., Castellote, Isabel, Tong, Jie Xin, Chandramohanadas, Rajesh, Chu, Trang Thi Thu, Shen, Wanxiang, Go, Mei Lin, de Cozar, Cristina, Crespo, Benigno

Source: ACS chemical biology. 16(11):2348-2372

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCRN628094767&indx=1&recIds=ETOCRN628094767

Leveraging the Aggregated Protein Dye YAT2150 for Malaria Chemotherapy.

Authors: Camarero-Hoyos, Claudia, Bouzón-Arnáiz, Inés, Avalos-Padilla, Yunuen, Fallica, Antonino Nicolò, Román-Álamo, Lucía, Ramírez, Miriam, Portabella, Emma, Cuspinera, Ona, Currea-Ayala, Daniela, Orozco-Quer, Marc, Ribera, Maria, Siden-Kiamos, Inga, Spanos, Lefteris, Iglesias, Valentín, Crespo, Benigno, Viera, Sara, Andreu, David, Sulleiro, Elena, Zarzuela, Francesc, Urtasun, Nerea

Source: Pharmaceutics; Oct2024, Vol. 16 Issue 10, p1290, 23p

Subject Terms: DRUG metabolism, DRUG therapy, PLASMODIUM falciparum, CYTOTOXINS, BINDING sites, PLASMODIUM

Substituted Aminoacetamides as Novel Leads for Malaria Treatment

Authors: Norcross, Neil R., Wilson, Caroline, Baragaña, Beatriz, Hallyburton, Irene, Osuna‐Cabello, Maria, Norval, Suzanne, Riley, Jennifer, Fletcher, Daniel, Sinden, Robert, Delves, Michael, Ruecker, Andrea, Duffy, Sandra, Meister, Stephan, Antonova‐Koch, Yevgeniya, Crespo, Benigno, de Cózar, Cristina, Sanz, Laura M., Gamo, Francisco Javier, Avery, Vicky M., Frearson, Julie A., Gray, David W., Fairlamb, Alan H., Winzeler, Elizabeth A., Waterson, David, Campbell, Simon F., Willis, Paul A., Read, Kevin D., Gilbert, Ian H.

Source: ChemMedChem. 14(14):1329-1335

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100085855848.0x000001&indx=1&recIds=ETOCvdc_100085855848.0x000001

Structures revealing mechanisms of resistance and collateral sensitivity of Plasmodium falciparum to proteasome inhibitors.

Authors: Hsu, Hao-Chi, Li, Daqiang, Zhan, Wenhu, Ye, Jianxiang, Liu, Yi Jing, Leung, Annie, Qin, Junling, Crespo, Benigno, Gamo, Francisco-Javier, Zhang, Hao, Cui, Liwang, Roth, Alison, Kirkman, Laura A., Li, Huilin, Lin, Gang

Source: Nature Communications; 12/14/2023, Vol. 14 Issue 1, p1-12, 12p

Subject Terms: PLASMODIUM falciparum, PROTEASOMES, PROTEASOME inhibitors, LIFE cycles (Biology), PLASMODIUM, DRUG target

High Throughput Screening to Identify Selective and Nonpeptidomimetic Proteasome Inhibitors As Antimalarials.

Authors: Mata-Cantero, Lydia, Xie, Stanley C., García, Mercedes, Coyle, Joanne, Fernandez, Raquel, Cabrera, Alvaro Cortes, Gillett, David L., Crespo, Benigno, Gamo, Francisco-Javier, Fernández, Esther, Tilley, Leann, Gomez-Lorenzo, Maria G.

Source: ACS Infectious Diseases; 6/11/2021, Vol. 7 Issue 6, p1818-1832, 15p

Repositioning and Characterization of 1‑(Pyridin-4-yl)pyrrolidin-2-one Derivatives as Plasmodium Cytoplasmic Prolyl-tRNA Synthetase Inhibitors.

Authors: Okaniwa, Masanori, Shibata, Akira, Ochida, Atsuko, Akao, Yuichiro, White, Karen L., Shackleford, David M., Duffy, Sandra, Lucantoni, Leonardo, Dey, Sumanta, Striepen, Josefine, Yeo, Tomas, Mok, Sachel, Aguiar, Anna Caroline C., Sturm, Angelika, Crespo, Benigno, Sanz, Laura M., Churchyard, Alisje, Baum, Jake, Pereira, Dhelio B., Guido, Rafael V. C.

Source: ACS Infectious Diseases; 6/11/2021, Vol. 7 Issue 6, p1680-1689, 10p

Design, synthesis and antimalarial evaluation of novel thiazole derivatives

Authors: Bueno, José María, Carda, Miguel, Crespo, Benigno, Cuñat, Ana Carmen, de Cozar, Cristina, León, María Luisa, Marco, J. Alberto, Roda, Nuria, Sanz-Cervera, Juan F.

Source: In Bioorganic & Medicinal Chemistry Letters 15 August 2016 26(16):3938-3944

P. falciparum In Vitro Killing Rates Allow to Discriminate between Different Antimalarial Mode-of-Action.

Authors: Sanz, Laura M.¹, Crespo, Benigno¹, De-Cózar, Cristina¹, Ding, Xavier C.², Llergo, Jose L.¹, Burrows, Jeremy N.², García-Bustos, Jose F.³, Gamo, Francisco-Javier¹ francisco-javier.b.gamo@gsk.com

Source: PLoS ONE. Feb2012, Vol. 7 Issue 2, p1-11. 11p.

Subject Terms: *PLASMODIUM falciparum, *ANTIMALARIALS, *DRUG therapy for malaria, *PARASITES, *DRUG metabolism -- Evaluation, *PROTOZOAN diseases, *BIOCHEMISTRY, *PARASITE life cycles

Novel Antimalarial Tetrazoles and Amides Active against the Hemoglobin Degradation Pathway in Plasmodium falciparum

Authors: Lawong, Aloysus, Gahalawat, Suraksha, Okombo, John, Striepen, Josefine, Yeo, Tomas, Mok, Sachel, Deni, Ioanna, Bridgford, Jessica L., Niederstrasser, Hanspeter, Zhou, Anwu, Posner, Bruce, Wittlin, Sergio, Gamo, Francisco Javier, Crespo, Benigno, Churchyard, Alisje, Baum, Jake, Mittal, Nimisha, Winzeler, Elizabeth, Laleu, Benoît, Palmer, Michael J., Charman, Susan A., Fidock, David A., Ready, Joseph M., Phillips, Margaret A.

Source: Journal of Medicinal Chemistry; March 2021, Vol. 64 Issue: 5 p2739-2761, 23p

Synthesis and Structure–Activity Relationship of Dual-Stage Antimalarial Pyrazolo[3,4-b]pyridines

Authors: Eagon, Scott, Hammill, Jared T., Sigal, Martina, Ahn, Kevin J., Tryhorn, Julia E., Koch, Grant, Belanger, Briana, Chaplan, Cory A., Loop, Lauren, Kashtanova, Anna S., Yniguez, Kenya, Lazaro, Horacio, Wilkinson, Steven P., Rice, Amy L., Falade, Mofolusho O., Takahashi, Rei, Kim, Katie, Cheung, Ashley, DiBernardo, Celine, Kimball, Joshua J., Winzeler, Elizabeth A., Eribez, Korina, Mittal, Nimisha, Gamo, Francisco-Javier, Crespo, Benigno, Churchyard, Alisje, García-Barbazán, Irene, Baum, Jake, Anderson, Marc O., Laleu, Benoît, Guy, R. Kiplin

Source: Journal of Medicinal Chemistry; October 2020, Vol. 63 Issue: 20 p11902-11919, 18p

Development of Chemical Entities Endowed with Potent Fast-Killing Properties against Plasmodium falciparum Malaria Parasites.

Authors: Matralis, Alexios N., Malik, Adnan, Penzo, Maria, Moreno, Inmaculada, Almela, Maria J., Camino, Isabel, Crespo, Benigno, Saadeddin, Anas, Ghidelli-Disse, Sonja, Rueda, Lourdes, Calderon, Felix, Osborne, Simon A., Drewes, Gerard, Böesche, Markus, Fernández-Álvaro, Elena, Martin Hernando, Jose Ignacio, Baker, David A.

Source: Journal of Medicinal Chemistry; 10/24/2019, Vol. 62 Issue 20, p9217-9235, 19p

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Development of Chemical Entities Endowed with Potent Fast-Killing Properties against Plasmodium falciparumMalaria Parasites

Authors: Matralis, Alexios N., Malik, Adnan, Penzo, Maria, Moreno, Inmaculada, Almela, Maria J., Camino, Isabel, Crespo, Benigno, Saadeddin, Anas, Ghidelli-Disse, Sonja, Rueda, Lourdes, Calderon, Felix, Osborne, Simon A., Drewes, Gerard, Böesche, Markus, Fernández-Álvaro, Elena, Martin Hernando, Jose Ignacio, Baker, David A.

Source: Journal of Medicinal Chemistry; October 2019, Vol. 62 Issue: 20 p9217-9235, 19p

Correction to The Discovery of Novel Antimalarial Aminoxadiazoles as a Promising Nonendoperoxide Scaffold

Authors: Sandoval, Elena, Lafuente-Monasterio, María José, Almela, María J., Castañeda, Pablo, Jiménez Díaz, María Belén, Martínez-Martínez, María S., Vidal, Jaume, Angulo-Barturen, Íñigo, Bamborough, Paul, Burrows, Jeremy, Cammack, Nicholas, Chaparro, María J., Coterón, José M., de Cozar, Cristina, Crespo, Benigno, Díaz, Beatriz, Drewes, Gerard, Fernández, Esther, Ferrer-Bazaga, Santiago, Fraile, María Teresa, Gamo, Francisco J., Ghidelli-Disse, Sonja, Gómez, Rubén, Haselden, John, Huss, Sophie, León, María Luisa, de Mercado, Jaime, Macdonald, Simon J. F., Martín Hernando, José Ignacio, Prats, Sara, Puente, Margarita, Rodríguez, Anne, de la Rosa, Juan C., Rueda, Lourdes, Selenski, Carolyn, Willis, Paul, Wilson, David M., Witty, Michael, Calderón, Félix

Source: Journal of Medicinal Chemistry; 20240101, Issue: Preprints

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