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Novel 6‐Morpholino‐9 H ‐purine Derivatives: Synthesis, Pharmacological and In Silico Evaluation
Author(s) -
Nadaf AfraQuasar A.,
Dixit Shruti,
Yaseen Mohammed,
Mantur Shivaraj,
Najare Mahesh S.,
Joshi Shrinivas,
Vootla Shyamkumar,
Khazi Imtiyaz Ahmed M.
Publication year - 2020
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.202001702
Subject(s) - chemistry , antioxidant , candida albicans , morpholino , antimicrobial , stereochemistry , enzyme , in vitro , purine , in silico , purine analogue , biochemistry , microbiology and biotechnology , biology , organic chemistry , zebrafish , gene
Abstract A series of novel N‐ 9 substituted 6‐morpholino‐9 H ‐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.