Mt KARI-IN-5

Mt KARI-IN-5 (compound 6c) 是一种结核分歧杆菌酮醇酸还原异构酶 I (MtbKARI) 的有效抑制剂 (Ki: 4.72 μM)。Mt KARI-IN-5 对 MtbH37Rv 的活性表现出抑制作用，其 MIC 值为 1.56 μM，细胞毒性较低，对 HEK 的 IC50 值大于 64 μg mL。

Mt KARI-IN-4 (compound 5c) is a highly effective inhibitor of Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI), demonstrating a Ki value of 5.48 μM. Additionally, Mt KARI-IN-4 displays inhibitory properties against Mtb H37Rv, with a minimum inhibitory concentration (MIC) of 0.78 μM. Importantly, this compound exhibits low levels of cytotoxicity, as evident from its half-maximal inhibitory concentration (IC 50 ) value of over 72 μg mL against human embryonic kidney cells (HEK) [1].

Mt KARI-IN-1 is a lead compound that demonstrates strong inhibitory activity towards Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI), with a Ki value of 3.06 μM [1].

Mt KARI-IN-2 (compound 5b) is a highly effective inhibitor of Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI), with a Ki value of 2.02 μM. This compound also exhibits inhibitory activity against Mtb H37Rv, with a MIC value of 0.78 μM. Moreover, Mt KARI-IN-2 demonstrates low cytotoxicity, as evidenced by a HEK IC 50 greater than 86 μg mL [1].