Design, Synthesis and Biological Evaluation of Novel Furan & Thiophene Containing Pyrazolyl Pyrazolines as Antimalarial Agents

Abstract

In search for novel compounds targeting Malaria, based on the in silico molecular docking binding affinity data, the novel furans containing pyrazolyl chalcones (3a-d) and pyrazoline derivatives (4a-d) were synthesized. The formation of the synthesized compound were confirmed by spectral analysis like IR, ¹H NMR, ¹³C NMR and mass spectrometry. Compounds with thiophene and pyrazoline ring 4b (0.47 μM), 4c (0.47 μM) and 4d (0.21 μM) exhibited excellent anti-malarial activity against Plasmodium falciparum compared with standard antimalarial drug Quinine (0.83 μM). To check the selectivity furthermore, compounds were tested for antimicrobial activity and none of the synthesized compound exhibited significant potency compared with the standard antibacterial drug Chloramphenicol and antifungal drug Nystatin respectively. So, it can be resolved that the produced compounds show selectively toward antimalarial activity and have the potential to be explored further.

Graphical Abstract

Keywords:

• Antimalarial
• antimicrobial
• chalcones
• pfENR inhibitor
• pyrazole-pyrazolines
• thiophene

Acknowledgements

Authors are thankful to Microcare laboratory and TRC, Surat, Gujarat for providing antimicrobial and antimalarial activities and Director, SAIF, Panjab University, Chandigarh for providing spectral data; Schrodinger Inc. for providing the software to perform the in silico study.

Disclosure statement

No potential conflict of interest was reported by the author(s).