ArticleJournal of medicinal chemistry2025
Design, Synthesis, and Biological Evaluation of Mono- and Diamino-Substituted Squaramide Derivatives as Potent Inhibitors of Mycobacterial Adenosine Triphosphate (ATP) Synthase.
Article in Journal of medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
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Who cites it
4 citing papers in PubMed.
- Novel Squaramides and Squaramates Containing a Five-Membered Heterocyclic Ring: Synthesis, Structure, and Cytotoxicity.International journal of molecular sciences · 2026Article
- Crystal structure of theActa crystallographica. Section E, Crystallographic communications · 2026Article
- Functionalized Cytisine Squaramides: Synthesis, Structural Elucidation, and Co-Crystallization.Molecules (Basel, Switzerland) · 2026Article
- Fair and Square: Design, Synthesis and Biological Evaluations of Squaric Acid Derivatives as Novel HDAC8 Inhibitors.ChemMedChem · 2026Article
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Authors and funding
14 authors.
Funding
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Abstract
Amides of squaric acid are new drug candidates with activity against mycobacteria. Like the approved drug bedaquiline, these compounds achieve efficacy by inhibiting mycobacterial ATP synthase. However, squaramides have a different binding site than bedaquiline and possess the potential to inhibit bedaquiline-resistant strains. We developed an optimized synthesis for monoamino-substituted squaric acid analogues. Guided by an atomic model of a squaramide compound bound to its target, we synthesized 31 new monoamino/diamino-substituted squaric acid derivates. The efficacy of these compounds was determined in whole-cell assays against
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