Need for new drugs to fight against tuberculosis (TB) is increasing day by day. In the present work we have taken a spiro compound (GSK 2200150A) reported by GSK as a lead and we modified the structure of the lead to study the antitubercular activity. For structure activity profiling twenty-one molecules have been synthesized, characterized and evaluated for their antimycobacterial potency against both active and dormant TB. Compound 06, 1-((4-methoxyphenyl)sulfonyl)-4′,5′-dihydrospiro[piperidine-4,7′-thieno[2,3-c]pyran] was found to be the most potent compound (MIC: 8.23 µM) in active TB and was less effective than the lead but more potent than standard first line drug ethambutol. It was also found to be more efficacious than Isoniazid and Rifampicin and equipotent as Moxifloxacin against dormant Mycobacterium tuberculosis (MTB). Compound 06 also showed good inhibitory potential against over expressed latent MTB enzyme lysine ε-amino transferase with an IC₅₀ of 1.04 ± 0.32 µM. This compound is a good candidate for drug development owing to potential against both active and dormant stages of MTB.

对抗结核病（TB）的新药需求日益增加。在目前的工作中，我们以GSK报告的螺环化合物（GSK 2200150A）作为铅，并修改了铅的结构以研究抗结核活性。对于结构活性分析，已合成，表征和评估了21个分子对活性和休眠TB的抗分枝杆菌效力。化合物06，1 - （（4-甲氧基苯基）磺酰基）-4'，5'-二氢螺[哌啶-4,7'-噻吩并[2,3- Ç[吡喃]是活性结核中最有效的化合物（MIC：8.23 µM），比铅无效，但比标准的一线药物乙胺丁醇更有效。还发现它比异烟肼和利福平更有效，并且与莫西沙星等效，对休眠的结核分枝杆菌（MTB）有效。化合物06对过表达的潜在MTB酶赖氨酸ε-氨基转移酶也显示出良好的抑制潜力，IC ₅₀为1.04±0.32 µM。该化合物由于对MTB活跃期和休眠期都有潜在的潜力，因此是药物开发的良好候选者。