Aims: The screening of antimycobacterial benzo[d]thiazole-2-carboxamides against ATP-phosphoribosyl transferase (ATP-PRTase) was conducted. Materials & methods: The antitubercular potential of compounds 1 and 2 against ATP-PRTase was assessed through the determination of half maximal effective concentration (EC50) and binding constant (Kd), as well as competitive inhibitory studies and studies of perturbation of secondary structure, molecular modeling and L-histidine complementation assay. Results & conclusion: Compounds 1n and 2a significantly inhibited ATP-PRTase as evidenced by their EC50 and Kd values and the perturbation of the secondary structure study. Compound 1n exhibited stronger competitive inhibition toward ATP compared with 2a. The inhibition of the growth of Mycobacterium tuberculosis by targeting the L-histidine biosynthesis pathway and molecular modeling studies further supported the inhibition of ATP-PRTase.

中文翻译：

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苯并[d]噻唑-2-甲酰胺作为抑制分枝杆菌 ATP 磷酸核糖基转移酶的新抗结核化学类型。

目的：针对 ATP-磷酸核糖基转移酶 (ATP-PRTase) 进行抗分枝杆菌苯并[d]噻唑-2-甲酰胺的筛选。材料和方法：通过测定半数最大有效浓度 (EC50) 和结合常数 (Kd)，以及竞争性抑制研究和二级结构扰动研究，评估了化合物 1 和 2 对 ATP-PRTase 的抗结核潜力，分子建模和 L-组氨酸互补测定。结果与结论：化合物 1n 和 2a 显着抑制 ATP-PRTase，这由它们的 EC50 和 Kd 值以及二级结构研究的扰动所证明。与 2a 相比，化合物 1n 对 ATP 表现出更强的竞争性抑制作用。