A series of thieno[2,3-d]pyrimidine alkyne Mannich base derivatives (7a-e, 8a-e) and thieno[2,3-d]pyrimidine 1,3,4-oxadiazole derivatives (9a-e, 10a-e) have been synthesized and evaluated for their neuroprotective and neurotoxicity activities where 9a, 10d displayed good neuroprotection 10.6 and 11.88 µg/mL respectively against the H₂O₂ induced cell death at the EC₅₀ values and 9b, 9d showed respective toxic effects on PC12 cells at CC₅₀ 86.12 and 94.16 µg/mL. Compounds 9a, 9e, 10a and 10b showed strong antibacterial activity against two gram positive (S. aureus, B. subtilis) and two gram-negative strains (E. coli, P. aeruginosa) and showed good binding affinities with C(30) carotenoid dehydrosqualene synthase, Gyrase A and LpxC. This is the first report for the demonstration of thieno[2,3-d] pyrimidine derivatives as promising neuroprotective agents against H₂O₂ induced neurotoxicity on PC12 cells.

一系列噻吩并[2,3- d ]嘧啶炔烃曼尼希碱衍生物（7a-e，8a-e）和噻吩并[2,3 - d ]嘧啶1,3,4-恶二唑衍生物（9a-e，10a- e）已合成并评估了它们的神经保护和神经毒性活性，其中9a，10d在EC ₅₀值下分别对H ₂ O ₂诱导的细胞死亡表现出良好的神经保护作用10.6和11.88 µg / mL ，而9b，9d则对H ₂ O ₂表现出了各自的毒性作用。 PC12细胞的CC ₅₀ 86.12和94.16 µg / mL。化合物9a，9e，10a和10b对两个革兰氏阳性菌（金黄色葡萄球菌，枯草芽孢杆菌）和两个革兰氏阴性菌（大肠杆菌，铜绿假单胞菌）表现出强大的抗菌活性，并与C（30）类胡萝卜素脱氢角鲨烯合酶，回旋酶A和LpxC表现出良好的结合亲和力。这是首次证明噻吩并[2,3-d]嘧啶衍生物作为有前途的抗H ₂ O ₂诱导的PC12细胞神经毒性的神经保护剂。