PlumX Metrics
Embed PlumX Metrics

Synthesis, In Silico Analysis, Antibacterial, Radical Scavenging and Antidiabetic Activities of Certain Bis-Azetidinones and Bis-Thiazolidinones

Pharmaceutical Chemistry Journal, ISSN: 1573-9031, Vol: 58, Issue: 1, Page: 62-73
2024
  • 1
    Citations
  • 0
    Usage
  • 2
    Captures
  • 0
    Mentions
  • 0
    Social Media
Metric Options:   Counts1 Year3 Year

Metrics Details

  • Citations
    1
    • Citation Indexes
      1
      • CrossRef
        1
  • Captures
    2

Article Description

A panel of 1,1-(phenylene)bis[3-chloro-4-(substituted phenyl)azetidin-2-ones] (4a-m) and 3,3′-(1,4-phenylene)bis[2-(substituted phenyl)thiazolidin-4-ones] (5a-m) were synthesized from Schiff base intermediates 3a-m, that were in turn prepared from reaction between p-phenylenediamine and substituted benzaldehydes. The structures of title compounds and intermediates were confirmed by IR, H NMR, C NMR and mass spectral data. The compounds were screened for antibacterial, DPPH radical scavenging and antidiabetic activities. Compounds 4f and 4a exhibited good antibacterial activity against Gram-positive bacteria, but none showed appreciable activity against Gram-negative bacteria. In DPPH scavenging assay, compounds 5f, 5e and 5a exhibited good activity. Compound 5a displayed highly significant antidiabetic activity in fructose-induced diabetes in rats. The molecular docking studies of bis-thiazolidinones with PPAR-ã revealed the fit with high binding affinity and good interactions. Docking of compound 5a was comparable to the standard drug pioglitazone. The in silico physicochemical, drug-likeness and ADME properties of title compounds were also performed and the majority of them displayed satisfactory results.

Bibliographic Details

Shreenivas R. Deshpande; Manappa T. Mandalamari; Prasad V. Malagi; Chandrashekhar V. M.

Springer Science and Business Media LLC

Pharmacology, Toxicology and Pharmaceutics

Provide Feedback

Have ideas for a new metric? Would you like to see something else here?Let us know