4.2 Article

Design, synthesis and biological evaluation of novel N,4-diphenylthiazol-2-amine derivatives

Journal

MEDICINAL CHEMISTRY RESEARCH
Volume 29, Issue 3, Pages 442-458

Publisher

SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-019-02495-2

Keywords

N,4-diphenylthiazol-2-amine; Antimicrobial; Anti-inflammatory; Ciprofloxacin; Fluconazole; Protein denaturation assay

Funding

  1. DST-INSPIRE, New Delhi, India [2016/IF160657]
  2. UGC-SRF

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Novel N,4-diphenylthiazol-2-amine derivatives were designed and synthesized employing Hantzsch method. The three-step reaction involved in the synthesis occurred at a faster rate with excellent yields in eco-friendly conditions. The synthesized derivatives were characterized by spectral techniques such as H-1 NMR, C-13 NMR, FT-IR and GCMS. Single-crystal X-ray diffraction studies also confirmed the formation of title compounds. These compounds were evaluated in vitro for their antimicrobial and anti-inflammatory activities. The results demonstrated that most of the tested compounds showed potent antifungal activity. Interestingly, these compounds also exhibited good anti-inflammatory and moderate antibacterial activity towards sensitive as well as resistant bacterial strains. In silico studies depicted their good binding affinity profile against S. aureus (PDB ID: 1AD4) and C. albicans (PDB ID: 1AI9). [GRAPHICS] .

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