Synthesis, Antibacterial, and Antioxidant Activity of N-Acyl Derivatives of Annelated 2-Aminothiophene

Isakhanyan, A. U.; Akopyan, N. Z.; Stepanyan, G. M.; Arakelyan, A. G.; Buniatyan, Zh. M.; Muradyan, R. E.; Panosyan, G. A.; Harutyunyan, А. А.

doi:10.1134/s1070363222110317

Cited by 1 publication

(1 citation statement)

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“…Moreover, the sulfur-containing compounds can engage in redox reactions, generating reactive oxygen species (ROS) and other free radicals that induce oxidative damage in microbial cells [15]. Additionally, the sulfur atom enables interaction with microbial proteins through noncovalent forces like hydrogen bonding, van der Waals interactions and hydrophobic interactions, thereby impeding essential microbial processes [16,17]. The antimicrobial activity of thiophene is further influenced by structural features, such as functional groups and substitution patterns on the thiophene ring [18][19][20].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Structural Determination, Docking Study and Bioactivity of Novel Thiophene Derivatives

Mahyavanshi,

Lokhandwala,

Pandya

et al. 2024

ajc

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The present study reveals 4-methyl-3-(propylamino)thiophene-2-carboxylic acid (Articaine acid) as precursor derivative to synthesize novel thiophene compounds to evaluate their biological activity. The synthesized compounds were subjected to comprehensive characterization techniques including mass spectra, NMR and IR spectroscopy, confirming their structural integrity. Their antimicrobial activity was assessed via minimum inhibitory concentration (MIC) assay against selected bacterial strains. The results emphasize the potential therapeutic applications of these thiophene analogues as efficacious antimicrobial agents, thereby encouraging further investigation. Molecular docking was used to examine thiophene derivative binding affinities on the S. aureus tyrosyl-tRNA synthetase protein and it was found that phenylethylamine derivatives had the highest binding affinity, followed by cyclohexyl methyl and benzylamine derivatives.

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