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Updated: Nov 5, 2025

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Design, synthesis and antimicrobial activity of novel 2-aminothiophene containing cyclic and heterocyclic moieties
Yahya I Asiri1, Abdullatif Bin Muhsinah2, Abdulrhman Alsayari2
1Department of Pharmacology, College of Pharmacy, King Khalid University, P.O. Box 960, Abha 61421, Saudi Arabia.
Abstract:
One of the major challenges in the community and healthcare was an impedance of pathogenic bacteria to antibiotics. This work developed 2-aminothiophene derivatives as novel antimicrobial agents. Various 2-aminothiophene derivatives (3a-f, 5a-c, 6a, b, 7, 8a, b and 9) with cyclic and heterocyclic moieties at 5-position were synthesized, and characterized using NMR, IR, and mass spectroscopic techniques. The newly synthesized compounds were evaluated for their antimicrobial activity against bacteria S. pneumoniae, B. subtilis, P. aeruginosa, E. coli, and fungi A. fumigatus, S. mracemosum, G. candidum, C. albicans. Compound 3a with OH group at para position of phenyl ring exhibited significant antibacterial activity stronger than that of the drug standards Ampicillin and Gentamicin. Compound 6b possess pyrazole ring and compound 9 bearing pyridine ring showed promising antifungal activity compare to the standard drug Amphotericin B. The remaining compounds exhibited good to moderate inhibitory activities. In summary, the results suggest that the compounds from 2-aminothiophene derivatives can be used as antimicrobial agents.
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