Jéssica Alves Nunes, Fabrícia Nunes da Silva, Elany Barbosa da Silva, Clara Andrezza Crisóstomo Bezerra Costa, Johnnatan Duarte de Freitas, Francisco Jaime Bezerra Mendonça-Junior, Miriam Aparecida Giardini, Jair Lage de Siqueira-Neto, James H. McKerrow, Thaiz Rodrigues Teixeira, Louis William Odeesho, Conor R. Caffrey, Sílvia Helena Cardoso and Edeildo Ferreira da Silva-Júnior
New J. Chem., 2023,47, 10127-10146
Abstract
Trypanosoma cruzi (Chagas diseases – also named American trypanosomiasis) and T. brucei (human African trypanosomiasis – HAT) negatively impact public health, being endemic in several countries and leading to thousands of deaths per year.
Javier Ramos-Soriano, Maisie Holbrow-Wilshaw, Eliza Hunt, Y. Jennifer Jiang, Pablo Peñalver, Juan C. Morales and M. Carmen Galan
Chem. Commun., 2024,60, 11520-11523
From themed collection:
ChemComm 60th Anniversary Collection
Abstract
Azobenzene ligands targeting G4 DNA exhibit subnanomolar antiparasitic activity against T. brucei and a remarkable selectivity index (IC50 MRC-5/T. brucei) of 2285-fold.
Angeliki-Sofia Foscolos, Richard L. Atherton, Maria Billia, Markos-Orestis Georgiadis, Nuno Santarém, Anabela Cordeiro da Silva, Martin C. Taylor, John M. Kelly, Theodora Calogeropoulou, Andrew Tsotinis, Thomas Mavromoustakos and Ioannis P. Papanastasiou
RSC Med. Chem., 2026, Advance Article
Abstract
New nitroheterocyclic adamantane amides display promising trypanocidal activity. The spacer length between the adamantylphenyl backbone and the nitroheterocyclic ring plays a crucial role in potency.
Ankush Banerjee, Tiffany A. Brisco, Sneha Ray, Arani Datta, Xiaoyu Zhang, Zhen Zhang, Alexander A. Busse, Hanspeter Niederstrasser, Krissty Sumida, Bruce A. Posner, Dawn M. Wetzel, Margaret A. Phillips and Myles W. Smith
Org. Biomol. Chem., 2024,22, 9413-9425
Abstract
We describe the development of a unified approach to the synthesis of all known 5/5-spiroindimicin (SPM) alkaloids and their biological evaluation as antiparasitic agents.
Arthur Toynton, Lori Ferrins, Harriet L. Newson, Melissa L. Sykes, Swapna Varghese, Nghi Nguyen, Stephanie Russell, Raphaël Rahmani, Jeremy Cheang, Gavin R. Flematti, Brian W. Skelton, Bilal Zulfiqar, Vicky M. Avery, Jonathan B. Baell and Matthew J. Piggott
RSC Med. Chem., 2025,16, 1654-1680
Abstract
The protozoan parasites Trypanosoma brucei and T. cruzi cause African sleeping sickness and Chagas disease, respectively. SAR for antitrypanosomal 2-[(phenylheteroaryl)ethyl]amides and ureas was expanded, identifying promising oxazoles and pyrazoles.