Novel isoxazole thiophene-containing compounds active against Mycobacterium tuberculosis.

• Tác giả: Arnab K Chatterjee, Gabrielle Martinez, Case W McNamara, Paridhi Sukheja, Kirsten Tolentino, Jasmine Webb, Baiyuan Yang
• Ngôn ngữ: eng
• Ký hiệu phân loại: 625.82 Brick and stone
• Thông tin xuất bản: England : Bioorganic & medicinal chemistry letters , 2025
• Bộ sưu tập: NCBI
• ID: 284584

Tóm tắt

Screening of the ChemDiv molecular library in cholesterol media against Mycobacterium tuberculosis (Mtb) H37Rv strain identified a novel isoxazole thiophene hit as a putative Rv1625c/Cya activator with a promising in vitro activity and good pharmacokinetic properties. Twenty-nine analogs were synthesized to assess the structure-activity relationships (SAR) to further improve potency. The most notable analog was P15, which showed an intramacrophage EC