New insights into the bacterial RNA polymerase inhibitor CBR703 as a starting point for optimization as an anti-infective agent.

Zhu, WeixingHaupenthal, JörgGroh, MatthiasFountain, MichelleHartmann, Rolf W2014-09-162014-09-162014-07New insights into the bacterial RNA polymerase inhibitor CBR703 as a starting point for optimization as an anti-infective agent. 2014, 58 (7):4242-5 Antimicrob. Agents Chemother.1098-65962482007710.1128/AAC.02600-14http://hdl.handle.net/10033/326174CBR703 was reported to inhibit bacterial RNA polymerase (RNAP) and biofilm formation, considering it to be a good candidate for further optimization. While synthesized derivatives of CBR703 did not result in more-active RNAP inhibitors, we observed promising antibacterial activities. These again correlated with a significant cytotoxicity toward mammalian cells. Furthermore, we suspect the promising effects on biofilm formation to be artifacts. Consequently, this class of compounds can be considered unattractive as antibacterial agents.enArchived with thanks to Antimicrobial agents and chemotherapyNew insights into the bacterial RNA polymerase inhibitor CBR703 as a starting point for optimization as an anti-infective agent.ArticleAntimicrobial agents and chemotherapy