Hit-to-lead optimization of a benzene sulfonamide series for potential antileishmanial agents

文献情報

出版日 2020-08-25

DOI 10.1039/D0MD00165A

インパクトファクター 0

著者

Paul J. Koovits, Marco A. Dessoy, An Matheeussen, Louis Maes, Guy Caljon, Leonardo L. G. Ferreira, Rafael C. Chelucci, Simone Michelan-Duarte, Adriano D. Andricopulo, Simon Campbell, Jadel M. Kratz, Charles E. Mowbray, Luiz C. Dias

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要旨

A series of benzene sulphonamides with good potency and selectivity against Leishmania spp. intracellular amastigotes was identified by high-throughput screening. Approximately 200 compounds were synthesized as part of a hit-to-lead optimization program. The potency of the series appears to be strongly dependent on lipophilicity, making the identification of suitable orally available candidates challenging due to poor pharmacokinetics. Despite not identifying a clinical candidate, a likely solvent exposed area was found, best exemplified in compound 29. Ongoing detailed mode-of-action studies may provide an opportunity to use target-based medicinal chemistry to overcome the issues with the current series.

掲載誌

RSC Medicinal Chemistry

CiteScore: 0

自己引用率: 0%

年間論文数: 0

Hit-to-lead optimization of a benzene sulfonamide series for potential antileishmanial agents

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RSC Medicinal Chemistry

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