Synthesis and antimicrobial evaluation of amino sugar-based naphthoquinones and isoquinoline-5,8-diones and their halogenated compounds

European Journal of Medicinal Chemistry
Flaviana Rf DiasAnna Claudia Cunha

Abstract

Antibiotic resistance has emerged as a serious global public health problem and lately very few antibiotics have been discovered and introduced into clinical practice. Therefore, there is an urgent need for the development of antibacterial compounds with new mechanism of action, especially those capable of evading known resistance mechanisms. In this work two series of glycoconjugate and non-glycoconjugate amino compounds derived from of isoquinoline-5,8-dione and 1,4-naphthoquinone and their halogenated derivatives were synthesized and evaluated for antimicrobial activity against Gram-positive (Enterococcus faecalis ATCC 29212, Staphylococcus aureus ATCC 25923, S. epidermidis ATCC 12228, S. simulans ATCC 27851) and Gram-negative bacteria (E. coli ATCC 25922, Proteus mirabilis ATCC 15290, K. pneumoniae ATCC 4352 and P. aeruginosa ATCC 27853) strains of clinical importance. This study revealed that glycoconjugate compounds derived from halogeno-substituted naphthoquinones were more active against Gram-negative strains, which cause infections whose treatment is even more difficult, according to the literature. These molecules were also more active than isoquinoline-5,8-dione analogues with minimum inhibitory concentration (MIC = ...Continue Reading

Citations

Dec 1, 2019·Chemical Biology & Drug Design·Nilüfer BayrakAmaç Fatih Tuyun
Jan 3, 2020·Organic & Biomolecular Chemistry·Ryan D KruschelFlorence O McCarthy
May 23, 2020·International Journal of Nanomedicine·Mostafa M GhorabAhmed A Askar
Jan 9, 2021·Chemical Record : an Official Publication of the Chemical Society of Japan ... [et Al.]·James M WoodEufrânio N da Silva Júnior
Feb 10, 2021·Biochemical and Biophysical Research Communications·Cui-Cui ChenYu-Jing Lu
Feb 23, 2019·Bioorganic & Medicinal Chemistry·Senyuan CaiNing Sun
Apr 25, 2019·Research in Microbiology·Lorine BéthencourtAude Herrera-Belaroussi
Feb 1, 2020·The Journal of Organic Chemistry·Andreja JakasIvanka Jerić

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