New insights into the bacterial RNA polymerase inhibitor CBR 703 as a 2 starting point for optimization as an anti - infective agent
نویسندگان
چکیده
Weixing Zhu, Jörg Haupenthal, Matthias Groh, Michelle Fountain and Rolf W. 4 Hartmann* b] 5 [a] Helmholtz Institute for Pharmaceutical Research Saarland (HIPS), Department of Drug Design 6 and Optimization and [b] Pharmaceutical and Medicinal Chemistry, Saarland University, Campus 7 C2_3, D-66123 Saarbrücken, Germany. [c] Helmholtz Centre for Infection Research, 8 Inhoffenstraße 7, Braunschweig 38124, Germany. 9 10
منابع مشابه
New insights into the bacterial RNA polymerase inhibitor CBR703 as a starting point for optimization as an anti-infective agent.
CBR703 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 promi...
متن کاملNew insights into the bacterial RNA polymerase inhibitor CBR 703 1 as a starting point for optimization as an anti - infective agent
1 Helmholtz Institute for Pharmaceutical Research Saarland (HIPS), Department of Drug Design 5 and Optimization and 2 Pharmaceutical and Medicinal Chemistry, Saarland University, Campus 6 C2.3, D-66123 Saarbrücken, Germany. 3 Helmholtz Centre for Infection Research, 7 Inhoffenstraße 7, 38124 Braunschweig, Germany. 8 * Corresponding author. Fax: (+49) 681 302 70308 E-mail: rolf.hartmann@helmholt...
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RNA polymerase inhibitors like the CBR class that target the enzyme's complex catalytic center are attractive leads for new antimicrobials. Catalysis by RNA polymerase involves multiple rearrangements of bridge helix, trigger loop, and active-center side chains that isomerize the triphosphate of bound NTP and two Mg(2+) ions from a preinsertion state to a reactive configuration. CBR inhibitors ...
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تاریخ انتشار 2014