Synthesis and Antibacterial Activity of Some Heterocyclic Chalcone Analogues Alone and in Combination with Antibiotics

Molecules

Thanh-Dao Tran¹  Thi-Thao-Nhu Nguyen¹  Tuong-Ha Do¹  Thi-Ngoc-Phuong Huynh¹  Cat-Dong Tran¹ 

[1] ¹Department of Medicinal Chemistry, School of Pharmacy, University of Medicine and Pharmacy at Ho Chi Minh City, 41 Dinh Tien Hoang, Dist. 1, Ho Chi Minh City 70000, Vietnam

关键词: chalcone;    heterocyclic chalcone analogues;    synthesis;    antibacterial;    synergitic activity;    antibiotics combination;    MRSA;   

DOI  :  10.3390/molecules17066684

来源: mdpi

【 摘 要 】

A series of simple heterocyclic chalcone analogues have been synthesized by Claisen Schmidt condensation reactions between substituted benzaldehydes and heteroaryl methyl ketones and evaluated for their antibacterial activity. The structures of the synthesized chalcones were established by IR and ¹H-NMR analysis. The biological data shows that compounds p₅, f₆ and t₅ had strong activities against both susceptible and resistant Staphylococcus aureus strains, but not activity against a vancomycin and methicillin resistant Staphylococcus aureus isolated from a human sample. The structure and activity relationships confirmed that compounds f₅, f₆ and t₅ are potential candidates for future drug discovery and development.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.