by Dichiara M, Simpson QJ, Quotadamo A, Jalani HB, Huang AX, Millard CC, Klug DM, Tse EG, Todd MH, Silva GD, da Silva Emery F, Carlson JE, Zheng S-L, VleminckxM, Matheeussen A, Caljon G, Pollastri MP, Sjö P, Perry B, Ferrins L. ACS Infectious Diseases 2023, 9(8):1470–1487. doi: 10.1021/acsinfecdis.3c00040
Summary: Existing treatments for visceral leishmaniasis have variable efficacy, significant toxicity, rising resistance, and limited oral bioavailability, which necessitates the development of novel and affordable therapeutics. The authors of this manuscript 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-5H-pyrrolo[1,2-a]imidazoles with improved absorption, distribution, metabolism, and elimination properties.
