Literature

Abstract

5-Methylphenanthridium derivatives were designed, synthesized and evaluated for their in vitro antibacterial activity and cell division inhibitory activity against various Gram-positive and -negative bacteria. Among them, compounds 5A2, 5B1, 5B2, 5B3, 5C1 and 5C2 displayed the best on-target antibacterial activity with an MIC value of 4µg/mL against B. subtilis ATCC9372 and S. pyogenes PS, showing over 2-fold better activity than sanguinarine. The SARs showed that the 5-methylphenanthridium derivatives with the alkyl side chains at the 2-postion, especially the straight alkyl side chains exerted better on-target antibacterial activity.

DOI： 10.1016/j.bmcl.2017.06.005

Synthesis and antibacterial activity of 5-methylphenanthridium derivatives as FtsZ inhibitors

Bioorganic & Medicinal Chemistry Letters 2017.0

Antibacterial activity of substituted 5-methylbenzo[c]phenanthridinium derivatives

Bioorganic & Medicinal Chemistry Letters 2012.0

Novel 5-methyl-2-phenylphenanthridium derivatives as FtsZ-targeting antibacterial agents from structural simplification of natural product sanguinarine

Bioorganic & Medicinal Chemistry Letters 2018.0

Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci

European Journal of Medicinal Chemistry 2021.0

Antibacterial activity of N -methylbenzofuro[3,2- b ]quinoline and N -methylbenzoindolo[3,2- b ]-quinoline derivatives and study of their mode of action

European Journal of Medicinal Chemistry 2017.0

3-Phenyl substituted 6,7-dimethoxyisoquinoline derivatives as FtsZ-targeting antibacterial agents