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      https://www.ias.ac.in/article/fulltext/jcsc/134/0007

    • Keywords

       

      Amides; Thiazoles; Arylamide derivatives; Zone of inhibition; Assays; Escherichia coli; Enterobacter aerogens.

    • Abstract

       

      In the present study, we are reporting the synthesis of a total eight derivatives of N-(5-acetyl-4-methylthiazol-2-yl) Arylamide derivatives (3a-h). The products obtained in good to excellent yield representsdrug-like molecules with a well-developed structure-activity relationship. All the synthesized compoundswere further subjected to chemical characterization (NMR, FTIR and elemental analysis) and further testedfor biological activities (antioxidant, antibacterial, antifungal and α-glucosidase). The anti-oxidant propertiesof compound 3h (IC50 ± SEM = 141.9 ± 1.12 μg/mL) were found maximum in comparison to the rest of thederivatives. The antibacterial results showed the compounds 3d and 3h as a significant bacterial inhibitor. Thesignificant fungicidal activity was observed by compound 3a with the zone of inhibition up to 24 mm whichin comparison with the results of positive control (Terbinafine). When the effect was observed on α-glucosidaseactivity, the highest enzyme inhibition activity was observed by 3h (IC50 ± SEM 134.4 ± 1.01 lμ/mL) followed by 3c (IC50 ± SEM = 157.3 ± 1.11 lμ/mL). The results were further supported by moleculardocking studies and the chemical stability of the derivatives was also performed by density functional theory(DFTs) calculations. The data revealed that most of the derivatives are multi-target ligands and can be used aslead molecules for the synthesis of derivatives for their further evaluation at molecular targets for thetreatment of specific diseases.

    • Graphical Abstract

       

      Synopsis This article reports the synthesis of a total of eight derivatives of N-(5-acetyl-4-methylthiazol-2-yl) Arylamide derivatives. The products obtained in good to excellent yield represents drug-like molecules with a well-developed structure-activity relationship.

    • Author Affiliations

       

      RABAIL UJAN1 HAFIZ MOHAMMAD KASHIF MAHMOOD2 PERVAIZ ALI CHANNAR3 SYEDA ABIDA EJAZ2 SHOMAILA SAEED3 AAMER SAEED3 AMNA SAEED2 MAMOONA RAFIQ3 KASHIF ALI CHANNAR4 HAFIZ ABDUL BARI INDHER5 HAMMAD ISMAIL6

      1. Dr. M A Kazi Institute of Chemistry, University of Sindh, Jamshoro 76080, Pakistan
      2. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan
      3. Department of Chemistry, Quaid-i-Azam University, Islamabad 45320, Pakistan
      4. Department of Oral and Maxillofacial Surgery, Institute of Dentistry, Liaquat University, Jamshoro 76080, Pakistan
      5. National Centre of Excellence in Analytical Chemistry, University of Sindh, Jamshoro 76080, Pakistan
      6. Department of Biochemistry and Biotechnology, University of Gujrat, Gujrat 50700, Pakistan
    • Dates

       
  • Journal of Chemical Sciences | News

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