Benzoxazoles, Phthalazinones, and Arylurea-Based Compounds with IMP Dehydrogenase-Independent Antibacterial Activity against Francisella tularensis

is the causative agent of tularemia and a potential biowarfare agent. The virulence of is decreased by deletion of , the gene encoding IMP dehydrogenase (IMPDH), suggesting that this enzyme is a target for antibacterial design. Here we report that growth is blocked by inhibitors of bacterial IMPDHs....

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Bibliographic Details
Published in:Antimicrobial agents and chemotherapy 2017-10, Vol.61 (10)
Main Authors: Gorla, Suresh Kumar, Zhang, Yan, Rabideau, Meaghan M, Qin, Aiping, Chacko, Shibin, House, Amanda L, Johnson, Corey R, Mandapati, Kavitha, Bernstein, Hannah M, McKenney, Elizabeth S, Boshoff, Helena, Zhang, Minjia, Glomski, Ian J, Goldberg, Joanna B, Cuny, Gregory D, Mann, Barbara J, Hedstrom, Lizbeth
Format: Article
Language:English
Subjects:
Animals
Anti-Bacterial Agents
Anti-Bacterial Agents - pharmacology
Benzoxazoles
Benzoxazoles - pharmacology
Cell Line
Electron Transport Complex I - genetics
Experimental Therapeutics
Francisella tularensis
Francisella tularensis - drug effects
Humans
IMP Dehydrogenase
IMP Dehydrogenase - antagonists & inhibitors
IMP Dehydrogenase - genetics
Mice
Microbial Sensitivity Tests
Phthalazines
Phthalazines - pharmacology
Structure-Activity Relationship
Tularemia - drug therapy
Tularemia - microbiology
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Summary:is the causative agent of tularemia and a potential biowarfare agent. The virulence of is decreased by deletion of , the gene encoding IMP dehydrogenase (IMPDH), suggesting that this enzyme is a target for antibacterial design. Here we report that growth is blocked by inhibitors of bacterial IMPDHs. Seventeen compounds from two different frameworks, designated the D and Q series, display antibacterial activities with MICs of
ISSN:0066-4804
1098-6596
DOI:10.1128/AAC.00939-17