Tuberculosis (TB) is a disease caused by Mycobacterium and usually attack the lung. Synthesis of new dipeptide derivatives attached to antitubercular active heterocyclic rings like pyrazine and 1,3,4-oxadiazole called ethyl 2-(2-(5-((pyrazin-2-ylamino) methyl)-1,3,4-oxadiazol-2-ylthio) acetamido) acetamido)-3-(4-hydroxyphenyl) propanoate (EPOGTP) and iodinated EPOGTP are reported. The compounds have been characterized by mass, FT-IR and ¹H NMR spectroscopy. Their in vitro investigation against Mycobacterium tuberculosis cell line indicated good IC₅₀value of 210 μg/ml for EPOGTP and 86 μg/ml for iodo-EPOGTP. For study the biodisriution, the direct radioiodination of EPOGTP with iodine-131 using mild oxidizing agent, N-Bromosuccinimide (NBS), was performed and optimized for obtaining the maximum radiochemical purity (97.3 ± 0.47%). Then, the in vivo biodistribution in healthy mice showed good accumulation of radioiodinated EPOGTP in lung of about 41.83 ± 0.23% (the percentage of injected dose per gram of organ) at 15 min post-injection. As a conclusion, the synthetized dipeptide and its iodinated derivative could be further evaluated as a potential antitubercular agents.

结核病 (TB) 是一种由分枝杆菌引起的疾病，通常会侵袭肺部。合成新的二肽衍生物，连接到抗结核活性杂环，如吡嗪和 1,3,4-恶二唑，称为乙基 2-(2-(5-((吡嗪-2-基氨基) 甲基)-1,3,4-恶二唑)-报道了2-基硫基)乙酰氨基)乙酰氨基)-3-(4-羟基苯基)丙酸酯(EPOGTP)和碘化EPOGTP。这些化合物已通过质量、FT-IR 和¹ H NMR 光谱进行表征。他们针对结核分枝杆菌细胞系的体外研究表明，EPOGTP 的IC ₅₀值为 210 μg/ml，碘-EPOGTP 的IC ₅₀值为 86 μg/ml。为了研究生物分解，EPOGTP 与碘 131 使用温和的氧化剂N的直接放射性碘化- 溴代琥珀酰亚胺 (NBS)，进行并优化以获得最大放射化学纯度 (97.3 ± 0.47%)。然后，健康小鼠的体内生物分布显示，在注射后 15 分钟，放射性碘化 EPOGTP 在肺中的良好积累约为 41.83 ± 0.23%（每克器官注射剂量的百分比）。总之，合成的二肽及其碘化衍生物可以进一步评估为潜在的抗结核药物。