Synthesis and anti-Staphylococcus aureus activity of 2-pyrazoline and 2-isoxazoline derivatives

Tran Ngoc Chau, Phung Bich Tuyen, Phan-Canh Trinh, Pham Ngoc Thach 2021. Ho Chi Minh City Journal of Medicine 25:2.


Background: Staphylococcus aureus is listed by WHO as one of the 12 antibiotic-resistant bacteria which are considered as major threat to human health. Research on novel active substances against these bacterial strains is critical.

Objectives: Synthesis and antibacterial effect evaluation of 2-pyrazoline, 2-isoxazoline derivatives

Methods: These derivatives were synthesized via 2 steps. Structure of synthetic compound were charaterized by IR, MS and NMR spectroscopy. Purity was checked by thin layer chromatography and NMR. Anti- Staphylococcus aureus activities were tested on two strains MSSA (ATCC 29213) and MRSA (ATCC 43300) by agar diffusion method.

Results: Ten substances were successfully synthesized: 2-pyrazoline derivatives (2a-2e) and 2-isoxazoline derivatives (3a-3e). Structure of these derivatives were confirmed by IR, MS and NMR. Among them, novel compound 3d has not been published in literature. 2-Isoxazoline derivatives showed a potential inhibitory effect against MSSA (MIC = 32 µg/mL). Substitution of methoxy group on benzen ring of 2-isoxazoline derivatives has a positive effect on the activity.