title: One-pot cascade synthesis and in vitro evaluation of anti-inflammatory and antidiabetic activities of S-methylphenyl substituted acridine-1,8-diones.
abstract: Various S-methylphenyl substituted acridine-1,8-dione series (4a-i) were synthesized through a one-pot cascade synthetic approach involving the reaction of 4-(methylthio)benzaldehyde and dimedone with a variety of amines as nitrogen source under reflux in ethanol. All the synthesized derivatives were characterized by using spectroscopic methods. In vitro evaluations of anti-inflammatory and antidiabetic efficacies of all the synthesized compounds were investigated. The anti-inflammatory results infer that the compounds 4c and 4d are showing excellent activity with an inhibition percentage of 80.58 ± 0.42, 81.72 ± 1.72 by membrane stabilization and 77.72 ± 0.76, 78.76 ± 0.81 by albumin denaturation methods, which is comparable with the standard diclofenac at a concentration of 100 μg/ml. Further, the antidiabetic assay revealed the moderate activity for the synthesized compounds at a concentration of 100 μg/ml with respect to their standard drug, acarbose.
authors.affiliation: Department of Chemistry, School of Advanced Sciences, VIT University, Vellore, Tamil Nadu, India.
authors.forename: Lavanya
authors.initials: L
authors.lastname: Mallu
authors.affiliation: Department of Chemistry, Thiruvalluvar University, Vellore, Tamil Nadu, India.
authors.forename: Dhakshanamurthy
authors.identifier: http://orcid.org/0000-0001-7591-4841
authors.initials: D
authors.lastname: Thirumalai
authors.affiliation: Department of Chemistry, School of Advanced Sciences, VIT University, Vellore, Tamil Nadu, India.
authors.forename: Indira Viswambaran
authors.initials: IV
authors.lastname: Asharani
mesh_terms: D000166:Acridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D020650:Combinatorial Chemistry Techniques; D006801:Humans; D007004:Hypoglycemic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000516:alpha-Amylases / Q000037:antagonists & inhibitors
chemical_list: D000166:Acridines; D000893:Anti-Inflammatory Agents; D007004:Hypoglycemic Agents; D000516:alpha-Amylases
keywords: 4-(methylthio)benzaldehyde; 8-diones; acridine-1; anti-inflammatory activity; antidiabetic activity; dimedone