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标题:Compounds with 1,3,4-oxadiazole and azinane appendages to evaluate enzymes inhibition applications supported by docking and BSA binding
时间:2018-12-06 21:34:39
DOI:10.1080/23312009.2018.1441597
作者:Azizur Rehman;Javed Iqbal;Muhammad Athar Abbasi;Sabahat Zahra Siddiqui;Hira Khalid
摘要:Compounds with 1,3,4-oxadiazole and azinane appendages to evaluate enzymes inhibition applications supported by docking and BSA bindingA series of molecules bearing multiple functional groups were synthesized to study their antibiotic effect against Gram-positive and Gram-negative bacteria and lipoxygenase activity as well. 2,4-Dimethylcarbolic acid (1) was refluxed with ethyl...
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目录:
  • Abstract: 
  • 1. Introduction
  • 2. Results and discussion
    • 2.1. AChE inhibition studies
    • 2.2. Urease inhibition studies
    • 2.3. Molecular docking
    • 2.4. BSA binding studies
  • 3. Conclusion
  • 4. Materials and methods
    • 4.1. Materials
    • 4.2. Synthesis of ethyl 1-(4-nitrophenylsulfonyl)piperidin-4-carboxylate (1)
    • 4.3. Synthesis of 1-(4-nitrophenylsulfonyl)piperidine-4-carbohydrazide (2)
  • 4.4. Synthesis of 5-(1-(4-nitrophenylsulfonyl)piperidin-4-yl)-1,3,4-oxadiazol-2-thiol (3)
    • 4.5. Synthesis of N-(substituted)-2-bromoacetamides (5a–p)
    • 4.6. General procedure for the synthesis of target compounds (6a–p)
    • 4.7. Acetyl cholinesterase inhibition assay
    • 4.8. Urease inhibition assay
    • 4.9. Molecular docking simulations
    • 4.10. BSA-synthesized compounds interactions using fluorescence measurements
    • 4.11. Spectral data of synthesized compounds
    • 4.11.1. 2-(5-(1-(4-Nitrophenylsulfonyl)piperidin-4-yl)-1,3,4-oxadiazol-2-ylthio)-N-phenylacetamide (6a)
      • 4.11.2. N-(2,4-dimethylphenyl)-2-(5-(1-(4-nitrophenylsulfonyl)piperidin-4-yl)-1,3,4-oxadiazol-2-ylthio)acetamide (6b)
      • 4.11.3. N-(3,4-dimethylphenyl)-2-(5-(1-(4-nitrophenylsulfonyl)piperidin-4-yl)-1,3,4-oxadiazol-2-ylthio)acetamide (6c)
      • 4.11.4. N-(3,5-dimethylphenyl)-2-(5-(1-(4-nitrophenylsulfonyl)piperidin-4-yl)-1,3,4-oxadiazol-2-ylthio)acetamide (6d)
    • 4.11.5. 2-(5-(1-(4-Nitrophenylsulfonyl)piperidin-4-yl)-1,3,4-oxadiazol-2-ylthio)-N-o-tolylacetamide (6e)
    • 4.11.6. 2-(5-(1-(4-Nitrophenylsulfonyl)piperidin-4-yl)-1,3,4-oxadiazol-2-ylthio)-N-m-tolylacetamide (6f)
    • 4.11.7. 2-(5-(1-(4-Nitrophenylsulfonyl)piperidin-4-yl)-1,3,4-oxadiazol-2-ylthio)-N-p-tolylacetamide (6g)
      • 4.11.8. Methyl 2-(2-(5-(1-(4-nitrophenylsulfonyl)piperidin-4-yl)-1,3,4-oxadiazol-2 ylthio)acetamido)benzoate (6h)
      • 4.11.9. N-(2-ethoxyphenyl)-2-(5-(1-(4-nitrophenylsulfonyl)piperidin-4-yl)-1,3,4-oxadiazol-2-ylthio)acetamide (6i)
      • 4.11.10. N-(2-ethylphenyl)-2-(5-(1-(4-nitrophenylsulfonyl)piperidin-4-yl)-1,3,4-oxadiazol-2-ylthio)acetamide (6j)
      • 4.11.11. N-(4-ethylphenyl)-2-(5-(1-(4-nitrophenylsulfonyl)piperidin-4-yl)-1,3,4-oxadiazol-2-ylthio)acetamide (6k)
      • 4.11.12. N-(4-ethoxyphenyl)-2-(5-(1-(4-nitrophenylsulfonyl)piperidin-4-yl)-1,3,4-oxadiazol-2-ylthio)acetamide (6l)
      • 4.11.13. N-(2-ethyl-6-methylphenyl)-2-(5-(1-(4-nitrophenylsulfonyl)piperidin-4-yl)-1,3,4-oxadiazol-2-ylthio)acetamide (6m)
      • 4.11.14. N-(2-ethoxyphenyl)-2-(5-(1-(4-nitrophenylsulfonyl)piperidin-4-yl)-1,3,4-oxadiazol-2-ylthio)acetamide (6n)
      • 4.11.15. N-benzyl-2-(5-(1-(4-nitrophenylsulfonyl)piperidin-4-yl)-1,3,4-oxadiazol-2-ylthio)acetamide (6o)
      • 4.11.16. N-(2-methyl-6-nitrophenyl)-2-(5-(1-(4-nitrophenylsulfonyl)piperidin-4-yl)-1,3,4-oxadiazol-2-ylthio)acetamide (6p)
  • Acknowledgement
  • Funding
  • References

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