Chroman-Schiff base derivatives as potential Anti-Tubercular Agents: In silico studies, Synthesis, and Biological evaluation.

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Tác giả: Fuzail Ahmad, Dhurgham Al-Fahad, Martha K Al-Zrkani, Husian Njem Hameed, Syed Misbahul Hasan, Danish Iqbal, Mehnaz Kamal, Samar Mujeeb, Marwah Al Shouber, Kuldeep Singh

Ngôn ngữ: eng

Ký hiệu phân loại: 133.594 Types or schools of astrology originating in or associated with a

Thông tin xuất bản: United States : Bioorganic chemistry , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 717113

Tuberculosis (TB) continues to pose a significant public health challenge worldwide. Hydrazide-containing compounds have demonstrated considerable potential as anti- tubercular agents. In this study, we designed, synthesized, and evaluated a series of chroman- Schiff base derivatives, integrating a chroman scaffold with substituted phenyl moieties, as potential therapeutic candidates against TB. In silico studies were conducted to assess the binding interactions of the synthesized derivatives, specifically their R- and S-isomers, with the tuberculosis target protein InhA (PDB ID: 1ZID). Molecular docking revealed that two R-isomer derivatives, SM-5A and SM-6A, exhibited superior binding affinities (-10.6 kcal/mol) compared to the reference ligand INH-NADH (-10.3 kcal/mol) and the natural substrate NADH (-7.5 kcal/mol). Molecular dynamics simulations confirmed the long-term stability of these compound-protein complexes over a 100 ns trajectory, further substantiating their potential as stable inhibitors. The structures of the synthesized derivatives were validated using spectroscopic techniques, including FTIR,
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