Synthesis, In silico studies and In vitro evaluation for antioxidant and antibacterial properties of diarylmethylamines: A novel class of structurally simple and highly potent pharmacophore

A series of novel diarylmethylamines were synthesized via simple three component condensation reaction. In vitro antibacterial activity of the synthesized compounds was assessed against Gram-positive and Gram-negative bacteria. Compound 1f containing phenyl and N-methyl piperazine moiety was found t...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:European journal of pharmaceutical sciences 2016-06, Vol.88, p.202-209
Hauptverfasser: Mahato, Sujit, Singh, Anuma, Rangan, Latha, Jana, Chandan K.
Format: Artikel
Sprache:eng
Schlagworte:
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:A series of novel diarylmethylamines were synthesized via simple three component condensation reaction. In vitro antibacterial activity of the synthesized compounds was assessed against Gram-positive and Gram-negative bacteria. Compound 1f containing phenyl and N-methyl piperazine moiety was found to be potent against both pathogenic bacteria with MIC value of 31μg/mL. Diarylmethylamine 1l containing sesamol and N-methyl piperazine units was found to be the most effective against Gram-positive bacteria with MIC value of 15μg/mL. The compound leads to the damage of the bacterial cell membrane which was demonstrated by flow cytometry (FC) and field emission scanning electron microscopy (FESEM). Radical scavenging activity of compounds 1l and 1m was found out to be comparable with that of standard antioxidant BHT. Further, in silico studies were carried out to calculate the physico-chemical parameter of the synthesized compounds. [Display omitted]
ISSN:0928-0987
1879-0720
DOI:10.1016/j.ejps.2016.03.004