ArticleResearch square2026
High-Throughput Screening Identifies Novel Antileishmanial Scaffolds and Reveals Cross-Species Activity of Structurally Diverse Compounds.
Article in Research square, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Authors and funding
8 authors.
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Abstract
Background: Leishmaniasis remains a neglected tropical disease with limited therapeutic options and a continued need for new and effective treatments. High-throughput phenotypic screening provides an approach for identifying chemically diverse compounds with antileishmanial activity that can serve as a starting point for drug development. This study further characterized compounds identified through a previous high-throughput phenotypic screen to prioritize promising antileishmanial chemical scaffolds and evaluate their potential for continued drug development. Methods: Compounds belonging to two enriched scaffolds, 1,4-diaryl-pyrazolo-pyridinone (1,4-DAPP) and pyrazolo-[5,1-c][1,2,4]triazine (PTZ), along with structurally diverse singleton compounds, were evaluated for antileishmanial activity across Results: 1,4-DAPP #9279817 and PTZ #9234527 were prioritized as lead compounds based on their combined antileishmanial activity and host-cell selectivity, exhibiting intracellular amastigote IC Conclusions: The 1,4-DAPP and PTZ scaffolds represent promising candidates for continued antileishmanial development. These findings support continued optimization of both scaffolds while emphasizing the importance of evaluating antileishmanial activity in disease-relevant parasite models.
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