Projects per year
Abstract
The leishmaniases are diseases that affect millions of people across the world, in particular visceral leishmaniasis (VL) which is fatal unless treated. Current standard of care for VL suffers from multiple issues and there is a limited pipeline of new candidate drugs. As such, there is a clear unmet medical need to identify new treatments. This paper describes the optimization of a phenotypic hit against Leishmania donovani, the major causative organism of VL. The key challenges were to balance solubility and metabolic stability while maintaining potency. Herein, strategies to address these shortcomings and enhance efficacy are discussed, culminating in the discovery of preclinical development candidate GSK3186899/DDD853651 (1) for VL.
Original language | English |
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Pages (from-to) | 1180-1202 |
Number of pages | 23 |
Journal | Journal of Medicinal Chemistry |
Volume | 62 |
Issue number | 3 |
Early online date | 20 Dec 2018 |
DOIs | |
Publication status | Published - 14 Feb 2019 |
Keywords
- Leishmaniasis
- visceral leishmaniasis
- anti-visceral leishmaniasis agents
- Cdc2-related kinase 12 (CRK12) inhibitor
- neglected diseases
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Projects
- 1 Finished
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A Translational Engine for Biomedical Discoveries (Strategic Grant)
1/01/13 → 30/09/15
Project: Research
Profiles
-
Read, Kevin
- Drug Discovery Unit - Professor & Personal Chair of Quantitative Pharmacology
Person: Academic