On-target, dual aminopeptidase inhibition provides cross-species antimalarial activity

Autor: Rebecca C. S. Edgar, Tess R. Malcolm, Ghizal Siddiqui, Carlo Giannangelo, Natalie A. Counihan, Matthew Challis, Sandra Duffy, Mrittika Chowdhury, Jutta Marfurt, Madeline Dans, Grennady Wirjanata, Rintis Noviyanti, Kajal Daware, Chathura D. Suraweera, Ric N. Price, Sergio Wittlin, Vicky M. Avery, Nyssa Drinkwater, Susan A. Charman, Darren J. Creek, Tania F. de Koning-Ward, Peter J. Scammells, Sheena McGowan

Publikováno v: mBio, Vol 15, Iss 6 (2024)

ABSTRACT 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 compound MMV1557817 is a selective, nanomolar inhibitor of both Plasmodium falciparum an

Externí odkaz: https://doaj.org/article/2d940180a1bd41efa98e153bebf7c041

Synthesis and Antimalarial Evaluation of Halogenated Analogues of Thiaplakortone A

Autor: Folake A. Egbewande, Brett D. Schwartz, Sandra Duffy, Vicky M. Avery, Rohan A. Davis

Publikováno v: Marine Drugs, Vol 21, Iss 5, p 317 (2023)

The incorporation of bromine, iodine or fluorine into the tricyclic core structure of thiaplakortone A (1), a potent antimalarial marine natural product, is reported. Although yields were low, it was possible to synthesise a small nine-membered libra

Externí odkaz: https://doaj.org/article/462bd368d90f4f7bb0725e71c68cfabb

Open Source Drug Discovery: Highly Potent Antimalarial Compounds Derived from the Tres Cantos Arylpyrroles

Autor: Alice E. Williamson, Paul M. Ylioja, Murray N. Robertson, Yevgeniya Antonova-Koch, Vicky Avery, Jonathan B. Baell, Harikrishna Batchu, Sanjay Batra, Jeremy N. Burrows, Soumya Bhattacharyya, Felix Calderon, Susan A. Charman, Julie Clark, Benigno Crespo, Matin Dean, Stefan L. Debbert, Michael Delves, Adelaide S. M. Dennis, Frederik Deroose, Sandra Duffy, Sabine Fletcher, Guri Giaever, Irene Hallyburton, Francisco-Javier Gamo, Marinella Gebbia, R. Kiplin Guy, Zoe Hungerford, Kiaran Kirk, Maria J. Lafuente-Monasterio, Anna Lee, Stephan Meister, Corey Nislow, John P. Overington, George Papadatos, Luc Patiny, James Pham, Stuart A. Ralph, Andrea Ruecker, Eileen Ryan, Christopher Southan, Kumkum Srivastava, Chris Swain, Matthew J. Tarnowski, Patrick Thomson, Peter Turner, Iain M. Wallace, Timothy N. C. Wells, Karen White, Laura White, Paul Willis, Elizabeth A. Winzeler, Sergio Wittlin, Matthew H. Todd

Publikováno v: ACS Central Science, Vol 2, Iss 10, Pp 687-701 (2016)

Externí odkaz: https://doaj.org/article/389f0d71ee2a4fb79f8bb1da8028bfae

Open Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond.

Autor: Wesley C Van Voorhis, John H Adams, Roberto Adelfio, Vida Ahyong, Myles H Akabas, Pietro Alano, Aintzane Alday, Yesmalie Alemán Resto, Aishah Alsibaee, Ainhoa Alzualde, Katherine T Andrews, Simon V Avery, Vicky M Avery, Lawrence Ayong, Mark Baker, Stephen Baker, Choukri Ben Mamoun, Sangeeta Bhatia, Quentin Bickle, Lotfi Bounaadja, Tana Bowling, Jürgen Bosch, Lauren E Boucher, Fabrice F Boyom, Jose Brea, Marian Brennan, Audrey Burton, Conor R Caffrey, Grazia Camarda, Manuela Carrasquilla, Dee Carter, Maria Belen Cassera, Ken Chih-Chien Cheng, Worathad Chindaudomsate, Anthony Chubb, Beatrice L Colon, Daisy D Colón-López, Yolanda Corbett, Gregory J Crowther, Noemi Cowan, Sarah D'Alessandro, Na Le Dang, Michael Delves, Joseph L DeRisi, Alan Y Du, Sandra Duffy, Shimaa Abd El-Salam El-Sayed, Michael T Ferdig, José A Fernández Robledo, David A Fidock, Isabelle Florent, Patrick V T Fokou, Ani Galstian, Francisco Javier Gamo, Suzanne Gokool, Ben Gold, Todd Golub, Gregory M Goldgof, Rajarshi Guha, W Armand Guiguemde, Nil Gural, R Kiplin Guy, Michael A E Hansen, Kirsten K Hanson, Andrew Hemphill, Rob Hooft van Huijsduijnen, Takaaki Horii, Paul Horrocks, Tyler B Hughes, Christopher Huston, Ikuo Igarashi, Katrin Ingram-Sieber, Maurice A Itoe, Ajit Jadhav, Amornrat Naranuntarat Jensen, Laran T Jensen, Rays H Y Jiang, Annette Kaiser, Jennifer Keiser, Thomas Ketas, Sebastien Kicka, Sunyoung Kim, Kiaran Kirk, Vidya P Kumar, Dennis E Kyle, Maria Jose Lafuente, Scott Landfear, Nathan Lee, Sukjun Lee, Adele M Lehane, Fengwu Li, David Little, Liqiong Liu, Manuel Llinás, Maria I Loza, Aristea Lubar, Leonardo Lucantoni, Isabelle Lucet, Louis Maes, Dalu Mancama, Nuha R Mansour, Sandra March, Sheena McGowan, Iset Medina Vera, Stephan Meister, Luke Mercer, Jordi Mestres, Alvine N Mfopa, Raj N Misra, Seunghyun Moon, John P Moore, Francielly Morais Rodrigues da Costa, Joachim Müller, Arantza Muriana, Stephen Nakazawa Hewitt, Bakela Nare, Carl Nathan, Nathalie Narraidoo, Sujeevi Nawaratna, Kayode K Ojo, Diana Ortiz, Gordana Panic, George Papadatos, Silvia Parapini, Kailash Patra, Ngoc Pham, Sarah Prats, David M Plouffe, Sally-Ann Poulsen, Anupam Pradhan, Celia Quevedo, Ronald J Quinn, Christopher A Rice, Mohamed Abdo Rizk, Andrea Ruecker, Robert St Onge, Rafaela Salgado Ferreira, Jasmeet Samra, Natalie G Robinett, Ulrich Schlecht, Marjorie Schmitt, Filipe Silva Villela, Francesco Silvestrini, Robert Sinden, Dennis A Smith, Thierry Soldati, Andreas Spitzmüller, Serge Maximilian Stamm, David J Sullivan, William Sullivan, Sundari Suresh, Brian M Suzuki, Yo Suzuki, S Joshua Swamidass, Donatella Taramelli, Lauve R Y Tchokouaha, Anjo Theron, David Thomas, Kathryn F Tonissen, Simon Townson, Abhai K Tripathi, Valentin Trofimov, Kenneth O Udenze, Imran Ullah, Cindy Vallieres, Edgar Vigil, Joseph M Vinetz, Phat Voong Vinh, Hoan Vu, Nao-Aki Watanabe, Kate Weatherby, Pamela M White, Andrew F Wilks, Elizabeth A Winzeler, Edward Wojcik, Melanie Wree, Wesley Wu, Naoaki Yokoyama, Paul H A Zollo, Nada Abla, Benjamin Blasco, Jeremy Burrows, Benoît Laleu, Didier Leroy, Thomas Spangenberg, Timothy Wells, Paul A Willis

Publikováno v: PLoS Pathogens, Vol 12, Iss 7, p e1005763 (2016)

A major cause of the paucity of new starting points for drug discovery is the lack of interaction between academia and industry. Much of the global resource in biology is present in universities, whereas the focus of medicinal chemistry is still larg

Externí odkaz: https://doaj.org/article/18b88a00726d44659ebd19c6f7c84d1b

Discovery and Structure–Activity Relationships of Quinazolinone-2-carboxamide Derivatives as Novel Orally Efficacious Antimalarials

Autor: Atsuko Ochida, Masahiro Kamaura, Angelika Sturm, Xue Chen, Karen L. White, Benoît Laleu, Binglin Wang, Benigno Crespo, Yuichiro Akao, Nobuo Cho, Gong Chen, Vicky M. Avery, Sergio Wittlin, Laura M. Sanz, Francis C. K. Chiu, Koen J. Dechering, David M. Shackleford, Kasiram Katneni, Sandra Duffy, Leonardo Lucantoni, Susan A. Charman

Publikováno v: Journal of Medicinal Chemistry. 64:12582-12602

A phenotypic high-throughput screen allowed discovery of quinazolinone-2-carboxamide derivatives as a novel antimalarial scaffold. Structure-activity relationship studies led to identification of a potent inhibitor 19f, 95-fold more potent than the o

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a2cf33a3e0cc4d27cbcc8fe60cf19f5e
https://doi.org/10.1021/acs.jmedchem.1c00441