novobiocin and Atrioventricular-Block

novobiocin has been researched along with Atrioventricular-Block* in 1 studies

Other Studies

1 other study(ies) available for novobiocin and Atrioventricular-Block

Article	Year
Replacement of cardiotoxic aminopiperidine linker with piperazine moiety reduces cardiotoxicity? Mycobacterium tuberculosis novel bacterial topoisomerase inhibitors. Bioorganic & medicinal chemistry, 2016, Jan-01, Volume: 24, Issue:1 Recently numerous non-fluoroquinolone-based bacterial type II topoisomerase inhibitors from both the GyrA and GyrB classes have been reported as antibacterial agents. Inhibitors of the GyrA class include aminopiperidine-based novel bacterial type II topoisomerase inhibitors (NBTIs). However, inhibition of the cardiac ion channel remains a serious liability for the aminopiperidine based NBTIs. In this paper we replaced central aminopiperidine linker with piperazine moiety and tested for its biological activity. We developed a series of twenty four compounds with a piperazine linker 1-(2-(piperazin-1-yl)ethyl)-1,5-naphthyridin-2(1H)-one, by following a multistep protocol. Among them compound 4-(2-(7-methoxy-2-oxo-1,5-naphthyridin-1(2H)-yl)ethyl)-N-(4-nitrophenyl)piperazine-1-carboxamide (11) was the most promising inhibitor with Mycobacterium tuberculosis (MTB) DNA gyrase enzyme supercoiling IC50 of 0.29±0.22μM, with a good MTB MIC of 3.45μM. These kind of compounds retains good potency and showed reduced cardiotoxicity compared to aminopiperidines. Topics: Animals; Antitubercular Agents; Atrioventricular Block; Cardiotoxicity; DNA Gyrase; Enzyme Assays; Ether-A-Go-Go Potassium Channels; Heart Rate; Mycobacterium tuberculosis; Naphthyridines; Novobiocin; Piperazines; Terfenadine; Topoisomerase II Inhibitors; Zebrafish; Zebrafish Proteins	2016

Article

Year

Replacement of cardiotoxic aminopiperidine linker with piperazine moiety reduces cardiotoxicity? Mycobacterium tuberculosis novel bacterial topoisomerase inhibitors.

Bioorganic & medicinal chemistry, 2016, Jan-01, Volume: 24, Issue:1

Recently numerous non-fluoroquinolone-based bacterial type II topoisomerase inhibitors from both the GyrA and GyrB classes have been reported as antibacterial agents. Inhibitors of the GyrA class include aminopiperidine-based novel bacterial type II topoisomerase inhibitors (NBTIs). However, inhibition of the cardiac ion channel remains a serious liability for the aminopiperidine based NBTIs. In this paper we replaced central aminopiperidine linker with piperazine moiety and tested for its biological activity. We developed a series of twenty four compounds with a piperazine linker 1-(2-(piperazin-1-yl)ethyl)-1,5-naphthyridin-2(1H)-one, by following a multistep protocol. Among them compound 4-(2-(7-methoxy-2-oxo-1,5-naphthyridin-1(2H)-yl)ethyl)-N-(4-nitrophenyl)piperazine-1-carboxamide (11) was the most promising inhibitor with Mycobacterium tuberculosis (MTB) DNA gyrase enzyme supercoiling IC50 of 0.29±0.22μM, with a good MTB MIC of 3.45μM. These kind of compounds retains good potency and showed reduced cardiotoxicity compared to aminopiperidines.

Topics: Animals; Antitubercular Agents; Atrioventricular Block; Cardiotoxicity; DNA Gyrase; Enzyme Assays; Ether-A-Go-Go Potassium Channels; Heart Rate; Mycobacterium tuberculosis; Naphthyridines; Novobiocin; Piperazines; Terfenadine; Topoisomerase II Inhibitors; Zebrafish; Zebrafish Proteins

2016