Ali Mohamed Ashraf, Shaharyar Mohammad
Department of Medicinal Chemistry, Alwar Pharmacy College, Alwar, Rajasthan 301030, India.
Bioorg Med Chem Lett. 2007 Jun 15;17(12):3314-6. doi: 10.1016/j.bmcl.2007.04.004. Epub 2007 Apr 6.
A series of oxadiazole mannich bases were synthesized by reacting oxadiazole derivatives, dapsone and appropriate aldehyde in the presence of methanol. The synthesized compounds were evaluated for antimycobacterial activity against M. tuberculosis H(37)Rv and INH resistant M. tuberculosis. Among the synthesized compounds, compound (4) 3-{2-furyl[4-(4-{2-furyl[5-(2-naphthyloxymethyl)-2-thioxo-2,3-dihydro-1,3,4-oxadiazol-3-yl]methylamino}phenylsulfonyl)anilino]methyl}-5-(2-naphthyloxymethyl)-2,3-dihydro-1,3,4-oxadiazole-2-thione was found to be the most promising compound active against M. tuberculosis H(37)Rv and isoniazid (INH) resistant M. tuberculosis with Minimum inhibitory concentration (MIC) 0.1 microM & 1.10 microM respectively.
通过使恶二唑衍生物、氨苯砜和适当的醛在甲醇存在下反应，合成了一系列恶二唑曼尼希碱。对合成的化合物进行了抗结核分枝杆菌活性评估，针对结核分枝杆菌H(37)Rv和耐异烟肼的结核分枝杆菌。在合成的化合物中，化合物(4) 3-{2-呋喃基[4-(4-{2-呋喃基[5-(2-萘氧基甲基)-2-硫代-2,3-二氢-1,3,4-恶二唑-3-基]甲基氨基}苯基磺酰基)苯胺基]甲基}-5-(2-萘氧基甲基)-2,3-二氢-1,3,4-恶二唑-2-硫酮被发现是最有前景的化合物，对结核分枝杆菌H(37)Rv和耐异烟肼(INH)的结核分枝杆菌具有活性，最低抑菌浓度(MIC)分别为0.1微摩尔和1.10微摩尔。
