@article{102689, keywords = {Infectious diseases, Parasites, Drug Discovery, Education, Trypanosoma cruzi, structure−activity relationships, Neglected tropical diseases (NTDs)}, author = {Abdulai Z and Agbo N and Anderson JI and Astley F and Chan B and Atkinson-Evans O and Avelar JL and Aparecida-Silva C and Bhardwaj K and Bowley WJ and Breitkreuz N and Canby R and Cartwright E and Clifford C and Cordell SA and Donker WJ and Driscoll J and Grady M and Higginbotham L and Hsu D and Hutchinson J and Imberg L and Jackson HF and Johns F and Jones E and Kalinin DV and Kardeşler C and Keal A and Keel L and Kim S and Knight P and Ködel JF and Kumeta L and Lee H and Le Roy S and Maccarone R and Mahmud M and Martin M and Nguyen I and Nolan CJ and Noyes L and Ntuwa ANW and Obarska W and Oldham O and Onyiuke E and Otter J and Page H and Patel D and Reid K and Samaddar K and Shabbir SM and Shevlin P and Sinclair-Wright C and Smithies A and Thomson AS and Tinker J and Uner A and Van Pelt N and Waddell E and Wagwa H and Walthorne C and Warner S and Winge T and Sum Wong N and Wysocki LJ and Yong CA and Zaheen Z and Matheeussen A and Caljon G and Amewu R and Bertram A and Biersack B and Friel C and Lima LM and Smith C and Wünsch B and Perry B and Cruz LR and Nortcliffe A}, title = {Collaborative Synthesis for Neglected Diseases through the Open Synthesis Network: Structure–Activity Relationships of Arylaminopyrazoles as Chagas Disease Treatments}, abstract = {
Neglected tropical diseases (NTDs) make up a diverse group of debilitating illnesses disproportionately affecting impoverished communities in tropical and subtropical regions. Despite their significant global health burden, they are often overshadowed by more prominent diseases, resulting in a critical lack of investment in the research and development of new treatments. A renewed focus on NTDs is, therefore, urgently needed, particularly in terms of novel therapeutic strategies. The Open Synthesis Network, launched by DNDi and partner institutions in 2016, is an innovation powerhouse that taps into the potential of students to help drive the discovery of new drugs for patients living with NTDs. We present the results of student-led work into the development of a series of aminopyrazoles for Chagas disease, a multisystemic disease caused by the Trypanosoma cruzi parasite. Seventy-four compounds were synthesized by undergraduate and postgraduate students from six universities from Brazil, Ghana, Germany, USA, and UK, illustrating that open innovation and collaboration for education can drive drug discovery forward. Early evaluation of the structure−activity relationships identified a range of potent hit compounds with selectivity for T. cruzi and no observable cytotoxicity.
}, year = {2025}, journal = {ACS Infectious Diseases}, pages = {1-14}, publisher = {American Chemical Society (ACS)}, issn = {2373-8227, 2373-8227}, url = {https://pubs.acs.org/doi/pdf/10.1021/acsinfecdis.5c00481?ref=article_openPDF}, doi = {10.1021/acsinfecdis.5c00481}, language = {ENG}, }