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

摘要

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.