One-pot cascade synthesis and in vitro evaluation of anti-inflammatory and antidiabetic activities of S-methylphenyl substituted acridine-1,8-diones

被引:23
作者
Mallu, Lavanya [1 ]
Thirumalai, Dhakshanamurthy [2 ]
Asharani, Indira Viswambaran [1 ]
机构
[1] VIT Univ, Sch Adv Sci, Dept Chem, Vellore, Tamil Nadu, India
[2] Thiruvalluvar Univ, Dept Chem, Vellore, Tamil Nadu, India
关键词
4-(methylthio)benzaldehyde; acridine-1; 8-diones; antidiabetic activity; anti-inflammatory activity; dimedone; DERIVATIVES; EFFICIENT; ACRIDINEDIONES; NANOPARTICLES; ACID;
D O I
10.1111/cbdd.12973
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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 100g/ml. Further, the antidiabetic assay revealed the moderate activity for the synthesized compounds at a concentration of 100g/ml with respect to their standard drug, acarbose.
引用
收藏
页码:520 / 526
页数:7
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