RSC Advances · 2022 · 32 citations · 37 references
PharmacyChemistryMedicinal ChemistryDrug DiscoveryOrganic ChemistrySynthetic Medicinal ChemistryLead Compound DesignLigand-based DesignMacrocycle SynthesisOral Antidiabetic AgentsHeterocycle FunctionalizationMedicinal Chemistry ApplicationsMolecular Docking AnalysisMolecular Docking OptimizationPyrrolidine SynthesisSpirocyclic Scaffolds
by the reaction of 1,2-dicarbonyl compounds and secondary amino acids is referred to as the 1,3-dipolar cycloaddition reaction. The reaction conditions were optimized to achieve excellent stereo- and regioselectivity. Shorter reaction time, simple work-up and excellent yields are the salient features of the present approach. Various spectroscopic methods and single crystal X-ray diffraction examinations of one example of compound 6i validated the stereochemistry of the expected products. The anti-diabetic activity of the newly synthesized spirooxindole derivatives was tested against the α-glucosidase and α-amylase enzymes. Compound 6i was found to exhibit potent inhibition activity against α-glucosidase and α-amylase enzymes which is further evidenced by molecular docking studies.
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Strategies for Innovation in Multicomponent Reaction Design
Bruce Ganem · Accounts of Chemical Research · 2009 · 1.2K citations · Full text
Structure-Based Design of Potent Non-Peptide MDM2 Inhibitors
Ke Ding, Yipin Lu, Zaneta Nikolovska‐Coleska et al. · Journal of the American Chemical Society · 2005 · 649 citations