Design, synthesis and antibacterial study of new potent and selective coumarin-chalcone derivatives for the treatment of tenacibaculosis

• Type: Article in International Scientific Journal
• Date: 2015

Authors

Vazquez Rodriguez, S (Author) Other; Lama Lopez, RL (Author) Other; Joao Matos, MJ (Author) Other; Armesto Quintas, G (Author) Other; Serra, S (Author) Other; Uriarte, E (Author) Other; Santana, L (Author) Other; Fernanda Borges (Author) FCUP; Munoz Crego, AM (Author) Other; Santos, Y (Author) Other

Journal

Title: Bioorganic and Medicinal Chemistry

Vol. 23

Pages: 7045-7052

ISSN: 0968-0896

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 32 Citations

Scopus - 36 Citations

Other information

Authenticus ID: P-00G-T87

DOI: 10.1016/j.bmc.2015.09.028

Abstract (EN): With the aim of finding new chemical entities selective for fish pathogens to avoid drug resistance in humans, a series of coumarin-chalcone hybrid compounds with different patterns of substitution were designed and synthesized. Their antibacterial activity was evaluated against important types of human bacteria strains (Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa) and against a fourteen strains of the marine pathogen Tenacibaculum maritimum, responsible for tenacibaculosis in fish, which is an important disease that causes great economical loss in the aquaculture industry. All the amino derivatives 5-12 presented high activity against different strains of T. maritimum, no activity against any of the three human pathogenic bacteria strains and no toxicity. Compounds 6, 7 and 11 were the most promising molecules. The most sensitive strains to these compounds were LL01 8.3.8 and LL01 8.3.1, being compound 11 up to 20 times more active than enrofloxacin. Therefore these scaffolds are good candidates for aquaculture treatments, avoiding possible drug resistance problems in humans.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 8