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6,161 results
  • Synthesis, SAR and in vitro therapeutic potentials of thiazolidine-2,4-diones. [Journal Article]
  • CCChem Cent J 2018 Dec 04; 12(1):129
  • Sucheta , Tahlan S, Verma PK
  • CONCLUSIONS: The synthesized compounds were screened for their in vitro antimicrobial potential against Gram (positive and negative) bacterial and fungal strains by tube dilution technique. In this series, compound 10 exhibited significant antimicrobial activity against B. subtilis and S. aureus with MIC = 4.2 × 10-2 µM/ml, compound 15 showed significant activity against K. pneumonia with MIC = 2.60 × 10-2 µM/ml and compound 4 displayed potent antibacterial activity against E. coli with MIC = 4.5 × 10-2 µM/ml. Compound 10 had most potent antifungal activity against C. albicans and A. niger with MIC = 4.2 × 10-2 µM/ml. Compounds 12 and 15 were found as most active antidiabetic agents having IC50 = 27.63 μg/ml and 22.35 μg/ml, respectively, using DPPH assay. Antioxidant activity results indicated that compounds 3 and 9 displayed good antioxidant agent with IC50 = 29.04 μg/ml and 27.66 μg/ml respectively, using α amylase assay.All the synthesized derivatives exhibited good antimicrobial, antidiabetic and antioxidant activities using specific methods then compared with mentioned standard drugs. Especially, compounds 3, 4, 9, 10, 12 and 15 displayed highest activity. Structure activity relationship demonstrated that presence of electron withdrawing group (o-NO2, p-Cl, p-Br) enhanced the antibacterial activity against E. coli as well as increased the antioxidant activity while the presence of electron releasing group (o/p-OCH3, 3,4,5-trimethoxy) enhanced the antibacterial activity against S. aureus, B. subtilis, S. typhi, K. pneumonia, C. albicans and A. niger as well as the antidiabetic activity.
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