Novel cyclohexyl-amides as potent antibacterials targeting bacterial type IIA topoisomerases

Autor:	Stephen Rittenhouse, Neil D. Pearson, Christopher Barfoot, Graham Elgin Jones, Timothy J. Miles, David L. Downie, Dongzhao Chen, Steven Dabbs, Jennifer Hoover, Roger Edward Markwell, Alan Joseph Hennessy, Jianzhong Huang, Michael N. Gwynn, Ilaria Giordano, Gerald Brooks, Hong Xiang, David T. Davies, Susanne Eyrisch, Pamela Brown
Rok vydání:	2011
Předmět:	medicine.drug_class Stereochemistry Clinical Biochemistry Antibiotics Pharmaceutical Science Microbial Sensitivity Tests Gram-Positive Bacteria Biochemistry Structure-Activity Relationship Dogs In vivo Gram-Negative Bacteria Drug Discovery medicine Animals Humans Topoisomerase II Inhibitors Potency Computer Simulation Mode of action Molecular Biology Binding Sites biology Chemistry Topoisomerase Organic Chemistry Haplorhini Amides Anti-Bacterial Agents Protein Structure Tertiary Rats DNA Topoisomerases Type II Mechanism of action biology.protein Molecular Medicine medicine.symptom
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 21:7483-7488
ISSN:	0960-894X
Popis:	As part of our wider efforts to exploit novel mode of action antibacterials, we have discovered a series of cyclohexyl-amide compounds that has good Gram positive and Gram negative potency. The mechanism of action is via inhibition of bacterial topoisomerases II and IV. We have investigated various subunits in this series and report advanced studies on compound 7 which demonstrates good PK and in vivo efficacy properties.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3810e692448006878f359f5ce7432ed6 https://doi.org/10.1016/j.bmcl.2011.09.114 Zobrazit plný text záznamu Full Text from ScienceDirect