![2,6-Di(thiophen-2-yl)dithieno[3,2-b:2',3'-d]thiophene structure](https://static.chemtradehub.com/structs/910/910788-24-8-5b70.webp "2,6-Di(thiophen-2-yl)dithieno[3,2-b:2',3'-d]thiophene structure")
2,6-Di(thiophen-2-yl)dithieno[3,2-b:2',3'-d]thiophene
CAS Number:
910788-24-8
Molecular Formula:
C16H8S5
Hit-to-lead optimization of a benzene sulfonamide series for potential antileishmanial agents
Literature Information
Publication Date
2020-08-25
DOI
10.1039/D0MD00165A
Impact Factor
0
Authors
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
View Original
Abstract
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.
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Source Journal
Recommended Compounds
N,N-Diethyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzamide
CAS Number:
325142-99-2
Molecular Formula:
C17H26BNO3
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