Novel 6-Morpholino-9H-purine Derivatives: Synthesis, Pharmacological and In Silico Evaluation

A series of novelN-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-2andPO-5have exhibited good activity against all the bacterial strains with MIC 4-8 mu g/mL whereasPO-5andPO-6exhibited strong inhibition of fungal strains (MIC: 2-4 mu g/mL). PP-5 has strongly inhibitedC. albicanswith MIC 2 mu g/mL which is similar to that of Fluconazole standard. The in silico studies performed onC. albicansindicated 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.