A small library of new benzothiazole clubbed oxadiazole-Mannich bases (M-1 to M-22) were synthesized and characterized by IR, NMR, Mass and Elemental analysis results. Molecular docking studies were done to assess the binding mode and interactions of synthesized hits at binding site of receptor Peroxisome proliferator-activated receptor, PPAR-γ or PPARG (PDB 1FM9). Among the synthesized compounds, nine compounds were selected on the basis of docking score and evaluated for their in vivo anti-diabetic activity using Oral Glucose Tolerance Test (OGTT) in normal rats followed by Streptozotocin (STZ) - induced diabetes. Results indicated that compound M-14 (161.39 ± 4.38) showed the highest reduction of blood glucose level comparable to that of the standard drug glibenclamide (140.29 ± 1.24) in STZ model. Other compounds exhibited moderate to good anti hyperglycaemic activity. ADME studies was done using Molinspiration online software, revealed that all compounds (except M-11) are likely to be orally active as they obeyed Lipinski’s rule of five.

合成了一个新的苯并噻唑球状恶二唑-曼尼希碱（M-1至M-22）的小文库，并通过IR，NMR，质量和元素分析结果进行了表征。进行了分子对接研究以评估受体过氧化物酶体增殖物激活的受体，PPAR-γ或PPARG（PDB 1FM9）的结合位点的结合模式和合成命中的相互作用。在合成的化合物中，根据对接得分选择了9种化合物，并通过口服葡萄糖耐量测试（OGTT）在正常大鼠中评估其体内抗糖尿病活性，然后评估链脲佐菌素（STZ）诱导的糖尿病。结果表明，化合物M-14（161.39±4.38）在STZ模型中显示出最高的血糖降低水平，与标准药物格列本脲（140.29±1.24）相当。其他化合物表现出中等至良好的抗高血糖活性。使用Molinspiration在线软件进行了ADME研究，结果表明，所有化合物（M-11除外）均符合Lipinski的5律，因此可能具有口服活性。