New 1-octanoyl-3-aryl thiourea derivatives: Solvent-free synthesis, characterization and multi-target biological activities

Authors

  • Fayaz Ali Larik Department of Chemistry, Quaid-i-Azam University, Islamabad 45320
  • Aamer Saeed Department of Chemistry, Quaid-i-Azam University, Islamabad 45320
  • Pervaiz Ali Channar Department of Chemistry, Quaid-i-Azam University, Islamabad 45320
  • Hammad Ismail Department of Biochemistry and Molecular Biology, University of Gujrat, Gujrat 50700
  • Erum Dilshad Department of Biochemistry, Quaid-i-Azam University, Islamabad 45320
  • Bushra Mirza Department of Biochemistry, Quaid-i-Azam University, Islamabad 45320

DOI:

https://doi.org/10.3329/bjp.v11i4.29059

Keywords:

Biological activity, Synthesis, Thiourea

Abstract

An efficient solvent-free synthesis of a 10-member library of octanoyl linked substituted aryl thioureas was accomplished successfully. The octanoyl isothiocyanate was freshly prepared in excellent yield and purity by the reaction of potassium thiocyanate with octanoyl chloride followed by removal of potassium chloride by filtration. The reaction of the latter with a series of ten different substituted anilines by stirring at 60-65°C lead to the formation of the title compounds. The in vitro antifungal activity of newly synthesized compounds was evaluated against Aspergillus niger, A. flavus and Fusarium solani strains of pathogenic fungi. Antibacterial assay was carried out against Gram positive (Staphylococcus aureus, Micrococcus luteus) and Gram negative bacterial strains (Escherichia coli, Enterobacter aerogens). Furthermore, anti-oxidant potential and enzyme inhibition studies against ?-amylase and butyryl cholinestrase were performed. The results obtained indicated moderate to excellent activities of most of the compounds whilst some derivatives showed potency higher than the standard used.

Video Clips of Methodology:

Antibacterial assay: 2 min 16 sec  Full Screen   Alternative

Enzyme inhibition: 1 min 27 sec  Full Screen   Alternative

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Author Biography

Aamer Saeed, Department of Chemistry, Quaid-i-Azam University, Islamabad 45320

Professor

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Published

2016-11-14

How to Cite

Larik, F. A., A. Saeed, P. A. Channar, H. Ismail, E. Dilshad, and B. Mirza. “New 1-Octanoyl-3-Aryl Thiourea Derivatives: Solvent-Free Synthesis, Characterization and Multi-Target Biological Activities”. Bangladesh Journal of Pharmacology, vol. 11, no. 4, Nov. 2016, pp. 894-02, doi:10.3329/bjp.v11i4.29059.

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Research Articles