Fragment-based design of symmetrical bis-benzimidazoles as selective inhibitors of the trimethoprim-resistant, type II R67 dihydrofolate reductase

…, A Mayence, TL Huang, JJ Vanden Eynde…

Index: Bastien, Dominic; Ebert, Maximilian C.C.J.C.; Forge, Delphine; Toulouse, Jacynthe; Kadnikova, Natalia; Perron, Florent; Mayence, Annie; Huang, Tien L.; Vanden Eynde, Jean Jacques; Pelletier, Joelle N. Journal of Medicinal Chemistry, 2012 , vol. 55, # 7 p. 3182 - 3192

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Citation Number: 9

Abstract

The continuously increasing use of trimethoprim as a common antibiotic for medical use and for prophylactic application in terrestrial and aquatic animal farming has increased its prevalence in the environment. This has been accompanied by increased drug resistance, generally in the form of alterations in the drug target, dihydrofolate reductase (DHFR). The most highly resistant variants of DHFR are known as type II DHFR, among which R67 ...