Dichiara, Maria;
Simpson, Quillon J;
Quotadamo, Antonio;
Jalani, Hitesh B;
Huang, Anson X;
Millard, Caroline C;
Klug, Dana M;
... Ferrins, Lori; + view all
(2023)
Structure-Property Optimization of a Series of Imidazopyridines for Visceral Leishmaniasis.
ACS Infectious Diseases
10.1021/acsinfecdis.3c00040.
(In press).
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Abstract
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-5H-pyrrolo[1,2-a]imidazoles with improved absorption, distribution, metabolism, and elimination properties.
| Type: | Article |
|---|---|
| Title: | Structure-Property Optimization of a Series of Imidazopyridines for Visceral Leishmaniasis |
| Location: | United States |
| Open access status: | An open access version is available from UCL Discovery |
| DOI: | 10.1021/acsinfecdis.3c00040 |
| Publisher version: | https://doi.org/10.1021/acsinfecdis.3c00040 |
| Language: | English |
| Additional information: | © 2023 The Authors. Published by American Chemical Society. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/) |
| Keywords: | leishmaniasis, neglected tropical diseases, structure−property optimization |
| UCL classification: | UCL UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy > Pharma and Bio Chemistry |
| URI: | https://discovery.ucl.ac.uk/id/eprint/10173450 |
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