Unveiling six potent and highly selective antileishmanial agents via the open source compound collection 'Pathogen Box' against antimony-sensitive and -resistant Leishmania braziliensis
Juliano A Souza Silva, Luiza G Tunes, Roney S Coimbra, David B Ascher, Douglas E Pires, Rubens L Monte-Neto
Biomedicine & Pharmacotherapy | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER | Published : 2021
Despite all efforts to provide new chemical entities to tackle leishmaniases, we are still dependent on a the limited drug arsenal, together with drawbacks like toxicity and drug-resistant parasites. Collaborative drug discovery emerged as an option to speed up the way to find alternative antileishmanial agents. This is the case of Medicines for Malaria Ventures - MMV, that promotes an open source drug discovery initiative to fight diseases worldwide. Here, we screened 400 compounds from 'Pathogen Box' (PBox) collection against Leishmania braziliensis, the main etiological agent of cutaneous leishmaniasis in Brazil. Twenty-three compounds were able to inhibit ≥ 80 % L. braziliensis growth at..View full abstract
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Awarded by National Health and Medical Research Council (NHMRC) of Australia
Awarded by CNPq
The authors thank the Medicines and Malaria Ventures (MMV) for providing the Pathogen Box and promoting collaborative drug discovery worldwide. We also thanks Dr. Marina Mourno Instituto Rene Rachou, Fundacao Oswaldo Cruz, for sharing some extra quantities of PBox compounds. We thank Dr. Heveline Silva, Department of Chemistry Universidade Federal de Minas Gerais, for her help on data mining from PBox compounds. JASS. received a scientific initiation (undergraduate) fellowship from Conselho Nacional de Desenvolvimento Cientffico e TecnolOgico CNPq, Brasil. This work was financed in part by the Coordenacno de Aperfeicoamento de Pessoal de Nivel Superior Brasil (Capes) with an award to LGT for a Ph.D. (Proap-Capes) scholarship. DBA was funded by an Investigator Grant from the National Health and Medical Research Council (NHMRC) of Australia [GNT1174405] and supported in part by the Victorian Government's OIS Pro-gram. RLMN is a CNPq Research Fellow (#310640/2017-2).