4.7 Article

Dihydrofolate reductase inhibitors for use as antimicrobial agents

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 195, Issue -, Pages -

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2020.112268

Keywords

Bacterial infections; DHFR; Mycobacterium tuberculosis; Escherichia coli; Staphylococcus aureus

Funding

  1. Science & Technology Department of Sichuan Province [2019YFSY0013]
  2. National Mega-project for Innovative Drugs [2019ZX09721001-001]
  3. National Natural Science Foundation of China [81973368]

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Drug-resistant bacteria pose an increasingly serious threat to mankind all over the world. However, the currently available clinical treatments do not meet the urgent demand.Therefore, it is desirable to find new targets and inhibitors to overcome the problems of antibiotic resistance. Dihydrofolate reductase (DHFR) is an important enzyme required to maintain bacterial growth, and hence inhibitors of DHFR have been proven as effective agents for treating bacterial infections. This review provides insights into the recent discovery of antimicrobial agents targeting DHFR. In particular, three pathogens, Escherichia coli (E. coli), Mycobacterium tuberculosis(Mtb) and Staphylococcus aureus(S. aureus), and research strategies are emphasized. DHFR inhibitors are expected to be good alternatives to fight bacterial infections. (C) 2020 Elsevier Masson SAS. All rights reserved.

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