Synthesis, Antibacterial Activity, and Molecular Docking Study of Bispyrazole-Based Derivatives as Potential Antibacterial Agent

Salman, Ghazwan Ali and Zinad, Dhafer S. and Mahal, Ahmed and Pratama, Mohammad Rizki Fadhil and Duan, Meiato and Alkhouri, Anas and Alamiery, Ahmed (2022) Synthesis, Antibacterial Activity, and Molecular Docking Study of Bispyrazole-Based Derivatives as Potential Antibacterial Agent. ChemistrySelect, 7 (4). pp. 1-6.

Text 1. Dokumen SLCT v7s4 2022.pdf Download (1MB)

Abstract

Development of novel antibacterial agents is one of most important aims in the field of medicinal chemistry and drug discovery. A new series of bispyrazole derivatives were synthesized with moderate to excellent yields ranging from 68 to 83 %. The structures of the newly synthesized compounds were confirmed using NMR, GC, IR techniques. The prepared derivatives were screened against Gram-positive bacteria (S. aureus and B. subtilis) and Gram-negative bacteria (E. coli and P. aeruginosa). All of the new compounds exhibited good to moderate antibacterial activity against Gram-positive and Gram-negative bacteria compared to trimethoprim. The bispyrazole bearing (triflouromethyl)benzene 8 d showed significant antibacterial inhibition against all bacteria tested and was found to be more active than trimethoprim in term of inhibition zone. Minimum inhibitory concentration (MIC) showed that the bispyrazoles bearing (methylsulfonyl)benzene 8 c and 4-chlorobenzen 8 e showed potent inhibition activity against Staphylococcus aureus and Bacillus subtilis while The bispyrazole bearing (triflouromethyl)benzene 8 d displayed strong inhibitory activity against S. aureus, B. subtilis, E. coli and P. aeruginosa compared to trimethoprim. Molecular docking was investigated for the active compounds and showed promising lead-like characters. These compounds could be employed as prospective lead compounds for the synthesis of novel antibacterial agents with highly potency.

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