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Synthesis, In Silico and Antifungal Studies of Novel Thiophene Analogues Containing Pyrazole Ring

[ Vol. 15 , Issue. 11 ]

Author(s):

Helmi M. Al-Maqtari, Joazaizulfazli Jamalis*, Subhash Chander, Hasnah M. Sirat , Shivalingegowda Naveen, Neratur K. Lokanath, Siti P.M. Bohari, Deepak P. Bhagwat and Murugesan Sankaranarayanan   Pages 1202 - 1210 ( 9 )

Abstract:


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.

Keywords:

Pyrazole, thiophene, antifungal, drug likeness, chalcone, synthesis.

Affiliation:

Department of Chemistry, Faculty of Science, Universiti Teknologi Malaysia, 81310 Johor Bahru, Johor, Department of Chemistry, Faculty of Science, Universiti Teknologi Malaysia, 81310 Johor Bahru, Johor, Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology & Science Pilani, Pilani Campus, Pilani-333031, Rajasthan, Department of Chemistry, Faculty of Science, Universiti Teknologi Malaysia, 81310 Johor Bahru, Johor, Department of Basic Sciences, School of Engineering and Technology, Jain University, Bangalore-562112, Department of Studies in Physics, Manasagangotri University of Mysore, Mysuru-570006, Department of Biotechnology and Medicinal Engineering, Faculty of Bioscience and Medical Engineering, Universiti Teknologi Malaysia, 81310 Johor Bahru, Johor, School of Pharmacy, Maharaja Agrasen University, Atal Shiksha Kunj, Village Kalujhanda, Solan, Himachal Pradesh 174103, Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology & Science Pilani, Pilani Campus, Pilani-333031, Rajasthan

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