A series of novel N‐ 9 substituted 6‐morpholino‐9H‐purine derivatives (PP 1–6; PO 1–6) were designed and synthesized via a multi‐step synthetic pathway. Spectroscopic techniques confirmed their chemical structures. The synthesized compounds were screened for in vitro antimicrobial, antioxidant and anti‐inflammatory activities. PP‐3 , PP‐5 , PP‐6 , PO‐2 and PO‐5 have exhibited good activity against all the bacterial strains with MIC 4–8 μg/mL whereas PO‐5 and PO‐6 exhibited strong inhibition of fungal strains (MIC: 2–4 μg/mL). PP‐5 has strongly inhibited C. albicans with MIC 2 μg/mL which is similar to that of Fluconazole standard. The in silico studies performed on C. albicans indicated that their mode of action is by the inhibition of dihydrofolate reductase enzyme. The anti‐inflammatory and antioxidant assays have shown that the halogen substituted derivatives have good anti‐inflammatory properties while the non halogen substituted derivatives exhibited good antioxidant profile.

中文翻译：

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新型6-Morpholino-9H-嘌呤衍生物：合成，药理和计算机模拟评估

设计并通过多步合成途径合成了一系列新颖的N- 9取代的6-吗啉代-9 H-嘌呤衍生物（PP 1–6； PO 1–6）。光谱技术证实了它们的化学结构。筛选合成的化合物的体外抗菌，抗氧化剂和抗炎活性。PP-3，PP-5，PP-6，PO-2和PO-5对MIC 4-8μg/ mL的所有细菌菌株均表现出良好的活性，而PO-5和PO-6对真菌菌株则表现出强烈的抑制作用（MIC：2-4μg/ mL）。PP-5强烈抑制MIC 2μg/ mL的白色念珠菌，与氟康唑标准品相似。在计算机上对白色念珠菌进行的研究表明，它们的作用方式是通过抑制二氢叶酸还原酶。抗炎和抗氧化剂测定表明，卤素取代的衍生物具有良好的抗炎特性，而非卤素取代的衍生物则具有良好的抗氧化剂特性。