{"id":13411,"date":"2025-11-05T13:41:00","date_gmt":"2025-11-05T13:41:00","guid":{"rendered":"https:\/\/www.sygnaturediscovery.com\/?post_type=journal-paper&p=13411"},"modified":"2026-01-29T15:43:43","modified_gmt":"2026-01-29T15:43:43","slug":"discovery-of-novel-fluorescent-amino-pyrazolines-that-detect-and-kill-mycobacterium-tuberculosis","status":"publish","type":"journal-paper","link":"https:\/\/www.sygnaturediscovery.com\/fr\/journal-paper\/discovery-of-novel-fluorescent-amino-pyrazolines-that-detect-and-kill-mycobacterium-tuberculosis\/","title":{"rendered":"Discovery of novel fluorescent amino-pyrazolines that detect and kill Mycobacterium tuberculosis"},"content":{"rendered":"\n

Yixin Cui, Alice Lanne, Sreenivas Avula, Mariwan A Hama Salih, Xudan Peng, Gavin Milne<\/strong>, Geraint Jones<\/strong>, John Ritchie<\/strong>, Yiming Zhao, Jon Frampton, Micky Tortorella, John S Fossey, Luke J Alderwick, Cleopatra Neagoie<\/p>\n\n\n\n

Abstract<\/strong><\/p>\n\n\n\n

The emergence of multidrug-resistant Mycobacterium tuberculosis (MDR-TB) necessitates novel therapeutics with distinct mechanisms. Here, we report amino-pyrazoline derivatives as a new class of dual-functional antimycobacterial agents, integrating potent bactericidal activity with fluorescence-based bacterial imaging. Initial screening identified AP-07 as a promising hit compound (MIC99<\/sub>: 40 \u03bcM against Mycobacterium smegmatis, 49 \u03bcM against Mycobacterium bovis BCG). Structure-based optimization led to the discovery of AP-02 and AP-05 as lead compounds, with enhanced activity (MIC99<\/sub>: 13-16 \u03bcM against M. smegmatis; 20-25 \u03bcM against M. bovis BCG). Additionally, spontaneous resistance assays detected no resistant colonies, suggesting a low risk of resistance development. Mechanistic studies confirmed Ag85C as the primary molecular target, disrupting late-stage mycolic acid biosynthesis and impairing cell wall integrity. Notably, pyrazoline derivatives exhibit intrinsic fluorescence, selectively labeling intracellular mycobacteria while remaining non-toxic to host macrophages, enabling real-time bacterial imaging. This work establishes fluorescent amino-pyrazolines as a promising foundation for next-generation antitubercular agents, bridging diagnostics and therapy in tuberculosis drug discovery.<\/p>\n\n\n\n

Ref: Eur J Med Chem 2025<\/a><\/p>\n\n\n\n

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