A series of GEQ analogues bearing pyrrolidinone or pyrrolidine cores were synthesized and evaluated against InhA, essential target for Mycobacterium tuberculosis (M.tb) survival. The compounds were also evaluated against M.tb H37Rv growth. Interestingly, some of the compounds, not efficient as InhA inhibitors, are active against M.tb with MICs up to 1.4 μM. In particular, compound 4b was screened with different M.tb mutated strains in order to identify the cellular target, but without success, suggesting a new possible mode of action.

中文翻译：

---

吡咯烷酮和吡咯烷衍生物：作为InhA和结核分枝杆菌抑制剂的评估

合成了一系列带有吡咯烷酮或吡咯烷核的GEQ类似物，并针对InhA（结核分枝杆菌（M.tb）存活的重要靶标）进行了评估。还评估了这些化合物对抗M.tb H37Rv的生长。有趣的是，某些化合物不能有效地发挥InhA抑制剂的作用，但对MIC高达1.4μM的M.tb具有活性。特别是，用不同的M.tb突变菌株筛选了化合物4b，以鉴定细胞靶标，但没有成功，提示了一种新的可能的作用方式。