Synthesis and Biological Screening of Thiophene Derivatives

Abstract

Heterocyclic compounds possessing the thiophene nucleus have attracted tremendous interest in the field of medicinal chemistry due to their promising pharmacological properties. A series of new thiophene derivatives were designed synthesized using an appropriate synthetic route. The suggested structures of the synthesized thiophene derivatives were confirmed using elemental analysis, ¹H-NMR, ¹³C-NMR, IR, and MS techniques. The synthesized new analogues were screened for their antibacterial activity against Streptococcus pneumoniae, Bacillis subtilis, Pseudomonas aeruginosa, Escherichia coli, and antifungal against Aspergillus fumigates, Syncephalastrum racemosum, Geotricum candidum, and Candida albicans. The in vitro antimicrobial study results revealed that these newly synthesized compounds exhibit potent antibacterial and antifungal activities, with that some compounds showed promising inhibition activity than the reference drugs. Compound 7 then selected for further cytotoxic activity against HCT-116 cell line revealed that compounds 7 (IC₅₀ = 11.13 μM) showed comparable cytotoxic activity to clinically used anticancer agent doxorubicin (IC₅₀ = 3.31 μM).

Graphical Abstract

Keywords:

• 2-Acetylthiophene
• heterocycles
• benzaldehyde
• antibacterial activity
• antifungal activity
• anticancer activity

Disclosure statement

The authors declare no conflict of interest.

Additional information

Funding

The Deanship of Scientific Research, King Khalid University is gratefully acknowledged for their financial support (Grant No. R. G. P. 2/26/42).