Synthesis and antibacterial activity of some heterocyclic chalcone analogues alone and in combination with antibiotics

• Published in: Molecules (Basel, Switzerland) Vol. 17; no. 6; pp. 6684 - 6696
• Main Authors: Tran, Thanh-Dao, Nguyen, Thi-Thao-Nhu, Do, Tuong-Ha, Huynh, Thi-Ngoc-Phuong, Tran, Cat-Dong, Thai, Khac-Minh
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 01.06.2012; MDPI
• Subjects: Anti-Bacterial Agents - chemical synthesis; Anti-Bacterial Agents - chemistry; Anti-Bacterial Agents - pharmacology; antibacterial; Antibiotics; antibiotics combination; Antimicrobial agents; chalcone; Chalcone - analogs & derivatives; Chalcone - chemical synthesis; Chalcone - chemistry; Chalcone - pharmacology; Drug Synergism; Electronic mail systems; heterocyclic chalcone analogues; Infectious diseases; Microbial Sensitivity Tests; Mortality; MRSA; Pharmacy; Staphylococcus aureus - drug effects; Staphylococcus infections; Structure-Activity Relationship; synergitic activity; synthesis; Vietnam
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules17066684

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.