Browsing by Author "Sreenivasa, Swamy"

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    Benzodioxole grafted spirooxindole pyrrolidinyl derivatives: synthesis, characterization, molecular docking and anti-diabetic activit
    (Royal Society of Chemistry, 2022-08-25) Nivetha, Narayanasamy; Martiz, Reshma Mary; Patil, Shashank M.; Ramu, Ramith; Sreenivasa, Swamy; Sivan, Velmathi
    A highly stereoselective, three-component method has been developed to synthesize pyrrolidine and pyrrolizidine containing spirooxindole derivatives. The interaction between the dipolarophile α,β-unsaturated carbonyl compounds and the dipole azomethine ylide formed in situ 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. © 2022 The Royal Society of Chemistry.
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    Sulfated magnesium zirconate catalyzed synthesis, antimicrobial, antioxidant, anti-inflammatory, and anticancer activity of benzo[d]thiazole-hydrazone analogues and its molecular docking
    (Elsevier B.V., 2021-09-20) Govindaiah, Shivaraja; Naha, Sanay; Madhuchakrapani Rao, Tadimety; Revanasiddappa B.C.; Srinivasa, Sudhanva M.; Parashuram, L; Velmathi, Sivan; Sreenivasa, Swamy
    A comprehensive demonstration of novel catalytic synthetic pathway using sulfated zirconia (solid acid catalyst) to generate a library of bioactive compounds precisely, the benzo[d]thiazole-hydrazone derivatives (4a-n). The compounds are characterized using ubiquitous spectroscopic techniques such as, IR, 1H and 13C NMR, HR-Mass. The set of molecules are screened in vitro biological activities namely, antimicrobial, antioxidant, anti-inflammatory and anticancer which are aptly supported by the molecular docking studies. Among the compounds, 4a and 4e are observed to be the most potent antibacterial agents where as 4a and 4c displayed significant antifungal activity. On the contrary, compounds 4e and 4j showed good antioxidant properties and 4b and 4j exhibited excellent anti-inflammatory activity. The compound 4d found to be a potent anti-cancer agent against tested human cancer cell lines MIAPaca2, HeLa, A549, and HCT116 (IC50 values of 19.09 ± 0.50, 19.93 ± 0.25, 7.76 ± 0.50, and 5.05 ± 0.25 μM respectively). Molecular docking studies were performed using DNA Gyrase, N-myristoyltransferase, COX-2, EGFR, HER2, and VEGFR2 proteins. Notably, compound 4d strongly binds to receptors EGFR and HER2 as inferred by their binding energies compared to standard inhibitors Gefitinib (EFGR), Lapatinib (EGFR), Afatinib (HER2), and Canertinib (HER2). © 2021