Article
Microbiology
Fidelia Ijeoma Uche, Xiaozhen Guo, Jude Okokon, Imran Ullah, Paul Horrocks, Joshua Boateng, Chenggang Huang, Wen-Wu Li
Summary: This study investigates the in vitro and in vivo antiplasmodial activities of BBIQ alkaloids and their analogues, showing promising results with significant anti-parasitic effects at low concentrations. Cycleanine and its semisynthetic analogues demonstrate improved potency and selectivity, with potential as leads for further drug development.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2021)
Article
Microbiology
James S. McCarthy, Azrin N. Abd-Rahman, Katharine A. Collins, Louise Marquart, Paul Griffin, Anne Kummel, Aline Fuchs, Cornelis Winnips, Vishal Mishra, Katalin Csermak-Renner, J. Prakash Jain, Preetam Gandhi
Summary: The new antimalarial compound cipargamin showed antimalarial activity in healthy volunteers infected with blood-stage Plasmodium falciparum, although some subjects experienced serious liver function changes during treatment. Further evaluation of the compound's hepatic safety profile is needed despite the promising antimalarial activity observed.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2021)
Article
Biology
Oluwole Solomon Oladeji, Abimbola Peter Oluyori, Adewumi Oluwasogo Dada
Summary: Morinda lucida, a plant traditionally used to treat malaria in Nigeria, has shown antiplasmodial properties in this study. The leaves and bark of Morinda lucida could be potential sources for developing effective antimalarial drugs.
SAUDI JOURNAL OF BIOLOGICAL SCIENCES
(2022)
Article
Microbiology
Ayman L. Hemasa, Matthias Mack, Kevin J. Saliba
Summary: This study found that two riboflavin analogues can inhibit the proliferation of malaria parasites by interfering with riboflavin metabolism and utilization. Roseoflavin, in particular, showed significant antimalarial activity in mice.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2022)
Article
Pharmacology & Pharmacy
Francisco Flavio Vieira de Assis, Jose Sousa de Almeida Junior, Tania Mara Pires Moraes, Fernando de Pilla Varotti, Camila Castilho Moraes, Adilson Sartoratto, Waldiney Pires Moraes, Antonio Humberto Hamad Minervino
Summary: This study evaluated the in vitro antimalarial activity and cytotoxicity of the hydroalcoholic extract of Juca (Libidibia ferrea). The results showed that the Juca extract exhibited significant antimalarial activity and no significant cytotoxicity.
Article
Biochemistry & Molecular Biology
Brodie L. Bailey, William Nguyen, Anna Ngo, Christopher D. Goodman, Maria R. Gancheva, Paola Favuzza, Laura M. Sanz, Francisco-Javier Gamo, Kym N. Lowes, Geoffrey I. McFadden, Danny W. Wilson, Benoit Laleu, Stephen Brand, Paul F. Jackson, Alan F. Cowman, Brad E. Sleebs
Summary: The study identified a triazolopyrimidine compound with good activity against Plasmodium falciparum and high selectivity against human cells, but faced challenges such as slow onset of action and low aqueous solubility. Further optimization is needed for its development as a potential partner in anti-malarial treatment.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Hao Zhang, John Ginn, Wenhu Zhan, Annie Leung, Yi J. Liu, Akinori Toita, Rei Okamoto, Tzu-Tshin Wong, Toshihiro Imaeda, Ryoma Hara, Mayako Michino, Takafumi Yukawa, Sevil Chelebieva, Patrick K. Tumwebaze, Jeremie Vendome, Thijs Beuming, Kenjiro Sato, Kazuyoshi Aso, Philip J. Rosenthal, Roland A. Cooper, Nigel Liverton, Michael Foley, Peter T. Meinke, Carl F. Nathan, Laura A. Kirkman, Gang Lin
Summary: Targeting the Plasmodium proteasome is a promising strategy to combat malaria, especially with the increasing reports of resistance to current therapies. In this study, we conducted structure-activity relationship studies on a macrocyclic scaffold and identified compound TDI-8414, which showed potent antiparasitic activity, high selectivity, improved solubility, and enhanced metabolic stability.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Parasitology
Gabriela Camila Krombauer, Karla de Sena Guedes, Felipe Fingir Banfi, Renata Rachide Nunes, Amanda Luisa da Fonseca, Ezequias Pessoa de Siqueira, Jessica Correa Bezerra Bellei, Kezia Katiani Gorza Scopel, Fernando de Pilla Varotti, Bruno Antonio Marinho Sanchez
Summary: This study evaluated the potential antimalarial activity of eight beta amino ketones in silico and in vitro. Compound 1 showed the highest activity and selectivity against P. falciparum, and its physicochemical properties met the criteria established by the Lipinski rule. It has the potential to be a drug prototype for antiplasmodial activity.
REVISTA DA SOCIEDADE BRASILEIRA DE MEDICINA TROPICAL
(2022)
Article
Biochemistry & Molecular Biology
Duc Hoang Lande, Abed Nasereddin, Arne Alder, Tim W. Gilberger, Ron Dzikowski, Johann Gruenefeld, Conrad Kunick
Summary: Malaria is a dangerous infectious disease for which novel antiplasmodial agents are needed due to parasite resistance. N-unsubstituted bisindolylcyclobutenediones were designed as potential drugs and showed promising antiplasmodial activity through molecular docking and synthesis.
Article
Chemistry, Multidisciplinary
Fabiana Volpe-Zanutto, Leticia Tiburcio Ferreira, Andi Dian Permana, Melissa Kirkby, Alejandro J. Paredes, Lalitkumar K. Vora, Amanda P. Bonfanti, Ives Charlie-Silva, Catarina Raposo, Mariana C. Figueiredo, Ilza M. O. Sousa, Andi Brisibe, Fabio Trindade Maranhao Costa, Ryan F. Donnelly, Mary Ann Foglio
Summary: Malaria affects over 200 million people annually and artemether and lumefantrine are the primary treatment options. Dissolving microneedles were developed to deliver the drugs intradermally, with studies in animals demonstrating significant efficacy.
JOURNAL OF CONTROLLED RELEASE
(2021)
Article
Chemistry, Medicinal
Camila Irabuena, Laura Scarone, Guilherme Eduardo de Souza, Anna Caroline Campos Aguiar, Giovana Rossi Mendes, Rafael Victorio Carvalho Guido, Gloria Serra
Summary: In recent years, progress in controlling malaria has slowed down. The World Health Organization has reported a modeling analysis predicting an increase in malaria morbidity and mortality in sub-Saharan Africa during the COVID-19 pandemic. Investigating the repurposing of old drugs could be a rapid way to discover new drugs. In this study, researchers prepared Nitazoxanide and analogs using two methodologies and evaluated their activity against P. falciparum 3D7.
MEDICINAL CHEMISTRY RESEARCH
(2022)
Article
Chemistry, Medicinal
Juliane Aparecida Marinho, Daniel Silqueira Martins Guimaraes, Nicolas Glanzmann, Giovana de Almeida Pimentel, Izabelle Karine da Costa Nunes, Henrique Marcelo Gualberto Pereira, Maribel Navarro, Fernando de Pilla Varotti, Adilson David da Silva, Clarice Abramo
Summary: In this study, molecular hybridization techniques were used to produce compound candidates with antiplasmodial activity for treating malaria infections by CQ-resistant strains. The candidates showed low cytotoxicity and selectiveness to parasites, with IQ5 and IQ6 demonstrating significant parasite growth inhibition in vivo. IQ6 also displayed interaction with ferriprotoporphyrin IX similar to CQ, suggesting promising potential for producing molecules with antiplasmodial activity.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Microbiology
Ryan Arey, Brad Reisfeld
Summary: A whole-body PBPK model was developed to predict the pharmacokinetic characteristics of artemisinin and its metabolite in blood, plasma, and tissues, showing good agreement with validation data. This tool is expected to improve dosing regimens by enabling a quantitative assessment of tissue-specific drug levels.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2021)
Article
Chemistry, Medicinal
Tatyana Almeida Tavella, Noeli Soares Melo da Silva, Natalie Spillman, Ana Carolina Andrade Vitor Kayano, Gustavo Capatti Cassiano, Adrielle Ayumi Vasconcelos, Antonio Pedro Camargo, Djane Clarys Baia da Silva, Diana Fontinha, Luis Carlos Salazar Alvarez, Leticia Tiburcio Ferreira, Kaira Cristina Peralis Tomaz, Bruno Junior Neves, Ludimila Dias Almeida, Daniel Youssef Bargieri, Marcus Vinicius Guimaraes de Lacerda, Pedro Vitor Lemos Cravo, Per Sunnerhagen, Miguel Prudencio, Carolina Horta Andrade, Stefanie Costa Pinto Lopes, Marcelo Falsarella Carazzolle, Leann Tilley, Elizabeth Bilsland, Julio Cesar Borges, Fabio Trindade Maranhao Costa
Summary: The natural compound violacein affects protein homeostasis in the malaria parasite, resulting in parasite growth inhibition. It could potentially be developed as a new anti-malarial drug due to its effects on the parasite's stress response.
ACS INFECTIOUS DISEASES
(2021)
Review
Infectious Diseases
Elahe Tajbakhsh, Tebit Emmanuel Kwenti, Parya Kheyri, Saeed Nezaratizade, David S. Lindsay, Faham Khamesipour
Summary: Although many indigenous plants in Africa have significant antiplasmodial and anti-malarial activity, progress in developing new anti-malarial drugs from African medicinal plants is slow. There is a need to scale up anti-malarial drug discovery in the African region.
Article
Biochemistry & Molecular Biology
Sharon Wein, Salma Ghezal, Corinne Bure, Marjorie Maynadier, Christian Perigaud, Henri J. Vial, Isabelle Lefebvre-Tournier, Kai Wengelnik, Rachel Cerdan
JOURNAL OF LIPID RESEARCH
(2018)
Article
Chemistry, Medicinal
Efres Belmonte-Reche, Marta Martinez-Garcia, Aurore Guedin, Michela Zuffo, Matilde Arevalo-Ruiz, Filippo Doria, Jenny Campos-Salinas, Marjorie Maynadier, Jose Juan Lopez-Rubio, Mauro Freccero, Jean-Louis Mergny, Jose Maria Perez-Victoria, Juan Carlos Morales
JOURNAL OF MEDICINAL CHEMISTRY
(2018)
Article
Biochemistry & Molecular Biology
Laurence Berry, Chun-Ti Chen, Maria E. Francia, Amandine Guerin, Arnault Graindorge, Jean-Michel Saliou, Maurane Grandmougin, Sharon Wein, Cherine Bechara, Juliette Morlon-Guyot, Yann Bordat, Marc-Jan Gubbels, Maryse Lebrun, Jean-Francois Dubremetz, Wassim Daher
CELLULAR AND MOLECULAR LIFE SCIENCES
(2018)
Article
Chemistry, Medicinal
Thomas Cheviet, Isabelle Lefebvre-Tournier, Sharon Wein, Suzanne Peyrottes
JOURNAL OF MEDICINAL CHEMISTRY
(2019)
Article
Chemistry, Medicinal
Olivier Berger, Stephanie Ortial, Sharon Wein, Severine Denoyelle, Francoise Bressolle, Thierry Durand, Roger Escale, Henri J. Vial, Yen Vo-Hoang
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2019)
Article
Multidisciplinary Sciences
Catherine Suarez, Gaelle Lentini, Raghavendran Ramaswamy, Marjorie Maynadier, Eleonora Aquilini, Laurence Berry-Sterkers, Michael Cipriano, Allan L. Chen, Peter Bradley, Boris Striepen, Martin J. Boulanger, Maryse Lebrun
NATURE COMMUNICATIONS
(2019)
Article
Cell Biology
Yen Vo-Hoang, Sergio Paiva, Leilei He, Sebastien Estaran, Yong Teng
Article
Chemistry, Medicinal
Thomas Cheviet, Sharon Wein, Gabriel Bourchenin, Manon Lagacherie, Christian Perigaud, Rachel Cerdan, Suzanne Peyrottes
JOURNAL OF MEDICINAL CHEMISTRY
(2020)
Article
Microbiology
Eleonora Aquilini, Marta Mendonca Cova, Shrawan Kumar Mageswaran, Nicolas Dos Santos Pacheco, Daniela Sparvoli, Diana Marcela Penarete-Vargas, Rania Najm, Arnault Graindorge, Catherine Suarez, Marjorie Maynadier, Laurence Berry-Sterkers, Serge Urbach, Pilar Ruga Fahy, Amandine N. Guerin, Boris Striepen, Jean-Francois Dubremetz, Yi-Wei Chang, Aaron P. Turkewitz, Maryse Lebrun
Summary: The study reveals that the mechanism of rhoptry secretion in Apicomplexa shares structural and genetic elements with ciliates, indicating a conserved secretion system adapted for defense in free-living unicellular eukaryotes and host cell injection in intracellular parasites. The formation of a rosette-shaped intramembranous particle embedded in the parasite apex plasma membrane is crucial for rhoptry exocytosis, which depends on non-discharge proteins conserved in Ciliata, Dinoflagellata, and Apicomplexa within the superphylum Alveolata.
NATURE MICROBIOLOGY
(2021)
Article
Chemistry, Medicinal
Alice Legru, Federica Verdirosa, Yen Vo-Hoang, Giusy Tassone, Filippo Vascon, Caitlyn A. Thomas, Filomena Sannio, Giuseppina Corsica, Manuela Benvenuti, Georges Feller, Remi Coulon, Francesca Marcoccia, Savannah Rowane Devente, Ezeddine Bouajila, Catherine Piveteau, Florence Leroux, Rebecca Deprez-Poulain, Benoit Deprez, Patricia Licznar-Fajardo, Michael W. Crowder, Laura Cendron, Cecilia Pozzi, Stefano Mangani, Jean-Denis Docquier, Jean-Francois Hernandez, Laurent Gavara
Summary: Metallo-beta-lactamases (MBLs) contribute to the resistance of Gram-negative bacteria to carbapenems. This study identifies a series of compounds with MBL inhibitory activity and strong synergistic effects against certain bacteria.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Microbiology
Sharon Wein, Nicolas Taudon, Marjorie Maynadier, Christophe Tran van Ba, Delphine Margout, Yann Bordat, Laurent Fraisse, Kai Wengelnik, Rachel Cerdan, Francoise Bressolle-Gomeni, Henri J. Vial
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2017)
Article
Chemistry, Multidisciplinary
Mohamed D. M. Traore, Vincent Zwick, Claudia A. Simoes-Pires, Alessandra Nurisso, Mark Issa, Muriel Cuendet, Marjorie Maynadier, Sharon Wein, Henri Vial, Helene Jamet, Yung-Sing Wong