Pyrazolopyrimidinediones are selective agents for Helicobacter pylori that suppress growth through inhibition of glutamate racemase (MurI).
Pyrazolopyrimidinediones are a novel series of compounds that inhibit growth of Helicobacter pylori specifically. Using a variety of methods, advanced analogues were shown to suppress the growth of H. pylori through the inhibition of glutamate racemase, an essential enzyme in peptidoglycan biosynthesis. The high degree of selectivity of the series for H. pylori makes these compounds attractive candidates for novel H. pylori-selective therapy.
Infection Discovery, Cancer and Infection Research Area, 35 Gatehouse Drive, Waltham, MA 02451, USA. Boudewijn.deJonge@astrazeneca.com
B L M
BL
de Jonge
A
A
Kutschke
M
M
Uria-Nickelsen
H D
HD
Kamp
S D
SD
Mills
D000591:Amino Acid Isomerases / Q000235:genetics / Q000378:metabolism*; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D001426:Bacterial Proteins / Q000235:genetics / Q000378:metabolism / Q000502:physiology; D015153:Blotting, Western; D002851:Chromatography, High Pressure Liquid; D004789:Enzyme Activation / Q000187:drug effects; D016480:Helicobacter pylori / Q000187:drug effects* / Q000201:enzymology* / Q000378:metabolism; D010457:Peptidoglycan / Q000378:metabolism; D011743:Pyrimidines / Q000737:chemistry*
D000900:Anti-Bacterial Agents; D001426:Bacterial Proteins; D010457:Peptidoglycan; D011743:Pyrimidines; D000591:Amino Acid Isomerases; C062292:glutamate racemase