Synthesis, in silico and antifungal studies of novel thiophene analogues containing pyrazole ring
Background: In the current study, a series of novel thiophene chalcones (3a-g) and pyrazole containing thiophene derivatives (6a-g) were designed as potential anti-fungal agents and evaluated in silico for drug-likeness behavior. Methods: The titled compounds were synthesized using Claisen–Schmidt r...
Saved in:
| Main Authors: | , , , , , , , , |
|---|---|
| Format: | Article |
| Published: |
Bentham Science Publishers B.V.
2018
|
| Subjects: | |
| Online Access: | http://eprints.utm.my/id/eprint/85669/ http://dx.doi.org/10.2174/1570180815666180328144325 |
| Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
| Institution: | Universiti Teknologi Malaysia |
| Summary: | Background: In the current study, a series of novel thiophene chalcones (3a-g) and pyrazole containing thiophene derivatives (6a-g) were designed as potential anti-fungal agents and evaluated in silico for drug-likeness behavior. Methods: The titled compounds were synthesized using Claisen–Schmidt reaction of 3-methyl-2-thiophenecarboxaldehyde (1) with several acetophenone derivatives (2a-g) followed by cyclization reactions using hydrazine hydrate to form new compounds (6a-g) in good to excellent yield. All the synthesized compounds were characterized by IR, 1H NMR, 13C NMR and Mass spectral analysis. All the synthesized chalcones (3a-g) and pyrazole derivatives (6a-g) were screened for antifungal potency using Candida albicans (MTCC 3958) and Aspergillus niger (MTCC 9933) using fluconazole as standard drug. Results & Conclusion: The assay results revealed interesting finding that, compound 6c showed significant activity against both the tested fungal strains. |
|---|