Year: 2023
Type: article
Abstract: High Resolution Image Download MS PowerPoint Slide Leishmaniasis is a collection of diseases caused by more than 20 Leishmania parasite species that manifest as either visceral, cutaneous, or mucocutaneous leishmaniasis. Despite the significant mortality and morbidity associated with leishmaniasis, it remains a neglected tropical disease. Existing treatments have variable efficacy, significant toxicity, rising resistance, and limited oral bioavailability, which necessitates the development of novel and affordable therapeutics. Here, we report on the continued optimization of a series of imidazopyridines for visceral leishmaniasis and a scaffold hop to a series of substituted 2-(pyridin-2-yl)-6,7-dihydro-5 H -pyrrolo[1,2- a ]imidazoles with improved absorption, distribution, metabolism, and elimination properties.
Source: ACS Infectious Diseases
Authors: Maria Dichiara, Quillon J. Simpson, Antonio Quotadamo, Hitesh B. Jalani, Anson X. Huang, Caroline C. Millard, Dana M. Klug, Edwin G. Tse, Matthew H. Todd, Daniel Gedder Silva, Flavio da Silva Emery, J. Eric Carlson, Shao-Liang Zheng, Margot Vleminckx, An Matheeussen, Guy Caljon, Michael P. Pollastri, Peter Sjö, Benjamin Perry, Lori Ferrins
Language: English
Field: Medicine
Domain: Health Sciences
Open Access status: hybrid
Estimated APC paid: $5,000
Funders: National Science Foundation, AstraZeneca, Médecins Sans Frontières, Fundação de Amparo à Pesquisa do Estado de São Paulo, Bundesministerium für Bildung und Forschung, Ministerie van Buitenlandse Zaken, Global Health Innovative Technology Fund, Drugs for Neglected Diseases initiative, Direktion für Entwicklung und Zusammenarbeit, National Institute of Allergy and Infectious Diseases
Awards: Lead optimization of hits identified from virtual and experimental screens of multiple industrial libraries DNDi, G3263080476, MRI: Acquisition of Single-Crystal Diffractometer for Small Molecule Crystallography and Cryosystem, Heterocyclic chemistry and epigenetic for the development of library of compounds for medicinal chemistry purposes.
OpenAlex ID: W4383484493