ChemInform Abstract: Potent and Selective Inhibitors of Helicobacter pylori glutamate Racemase (MurI): Pyridodiazepine Amines.

ChemInform ◽  
2009 ◽  
Vol 40 (26) ◽  
Author(s):  
Bolin Geng ◽  
et al. et al.
Keyword(s):  
Helicobacter Pylori ◽  
Selective Inhibitors ◽  
Glutamate Racemase

Potent and selective inhibitors of Helicobacter pylori glutamate racemase (MurI): Pyridodiazepine amines

2009 ◽  
Vol 19 (3) ◽  
pp. 930-936 ◽  
Author(s):  
Bolin Geng ◽  
Gregory Basarab ◽  
Janelle Comita-Prevoir ◽  
Madhusudhan Gowravaram ◽  
Pamela Hill ◽  
...  
Keyword(s):  
Helicobacter Pylori ◽  
Selective Inhibitors ◽  
Glutamate Racemase

scholarly journals Selective Inhibitors of Helicobacter pylori Methylthioadenosine Nucleosidase and Human Methylthioadenosine Phosphorylase

2019 ◽  
Vol 62 (7) ◽  
pp. 3286-3296 ◽  
Author(s):  
Rajesh K. Harijan ◽  
Oskar Hoff ◽  
Rodrigo G. Ducati ◽  
Ross S. Firestone ◽  
Brett M. Hirsch ◽  
...  
Keyword(s):  
Helicobacter Pylori ◽  
Selective Inhibitors ◽  
Methylthioadenosine Phosphorylase

Theoretical Analysis of the Catalytic Mechanism of Helicobacter pylori Glutamate Racemase

2012 ◽  
Vol 116 (41) ◽  
pp. 12406-12414 ◽  
Author(s):  
Edgar Mixcoha ◽  
Mireia Garcia-Viloca ◽  
José M. Lluch ◽  
Àngels González-Lafont
Keyword(s):  
Helicobacter Pylori ◽  
Theoretical Analysis ◽  
Catalytic Mechanism ◽  
Glutamate Racemase

scholarly journals Pyridodiazepine Amines Are Selective Therapeutic Agents for Helicobacter pylori by Suppressing Growth through Inhibition of Glutamate Racemase but Are Predicted To Require Continuous Elevated Levels in Plasma To Achieve Clinical Efficacy

2015 ◽  
Vol 59 (4) ◽  
pp. 2337-2342 ◽  
Author(s):  
Boudewijn L. M. de Jonge ◽  
Amy Kutschke ◽  
Joseph V. Newman ◽  
Michael T. Rooney ◽  
Wei Yang ◽  
...  
Keyword(s):  
Helicobacter Pylori ◽  
Therapeutic Agents ◽  
Infection Model ◽  
Content Type ◽  
Peptidoglycan Biosynthesis ◽  
Glutamate Racemase ◽  
Mouse Infection Model ◽  
Exposure Levels ◽  
H Pylori ◽  
Extended Exposure

ABSTRACTA pyridodiazepine amine inhibitor ofHelicobacter pyloriglutamate racemase (MurI) was characterized. The compound was selectively active againstH. pylori, and growth suppression was shown to be mediated through the inhibition of MurI by several methods. In killing kinetics experiments, the compound showed concentration-independent activity, with about a 2-log loss of viability in 24 h. A demonstration of efficacy in a mouse infection model was attempted but not achieved, and this was attributed to the failure to attain extended exposure levels above the MIC for >95% of the time. This index and magnitude were derived from pharmacokinetic-pharmacodynamic (PK-PD) studies with amoxicillin, another inhibitor of peptidoglycan biosynthesis that showed slow killing kinetics similar to those of the pyridodiazepine amines. These studies indicate that MurI and other enzymes involved in peptidoglycan biosynthesis may be less desirable targets for monotherapy directed againstH. pyloriif once-a-day dosing is required.

scholarly journals Identification of selective inhibitors of Helicobacter pylori IMPDH as a targeted therapy for the infection

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Kapil Juvale ◽  
Gayathri Purushothaman ◽  
Vijay Singh ◽  
Althaf Shaik ◽  
Srimadhavi Ravi ◽  
...  
Keyword(s):  
Helicobacter Pylori ◽  
Targeted Therapy ◽  
Selective Inhibitors

scholarly journals Pyrazolopyrimidinediones Are Selective Agents for Helicobacter pylori That Suppress Growth through Inhibition of Glutamate Racemase (MurI)

2009 ◽  
Vol 53 (8) ◽  
pp. 3331-3336 ◽  
Author(s):  
B. L. M. de Jonge ◽  
A. Kutschke ◽  
M. Uria-Nickelsen ◽  
H. D. Kamp ◽  
S. D. Mills
Keyword(s):  
Helicobacter Pylori ◽  
Peptidoglycan Biosynthesis ◽  
Glutamate Racemase ◽  
Selective Agents ◽  
Essential Enzyme ◽  
H Pylori ◽  
Selective Therapy ◽  
High Degree

ABSTRACT 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.

The rod-to-coccoid body transformation in cultures of Helicobacter pylori

1990 ◽  
Vol 48 (3) ◽  
pp. 626-627
Author(s):  
A. R. Crooker ◽  
W. G. Kraft ◽  
T. L. Beard ◽  
M. C. Myers
Keyword(s):  
Helicobacter Pylori ◽  
Growth Cycle ◽  
Negative Bacterium ◽  
Body Formation ◽  
Coccoid Form ◽  
Spiral Form ◽  
Prolonged Culture ◽  
H Pylori ◽  
Upper Gastrointestinal

Helicobacter pylori is a microaerophilic, gram-negative bacterium found in the upper gastrointestinal tract of humans. There is strong evidence that H. pylori is important in the etiology of gastritis; the bacterium may also be a major predisposing cause of peptic ulceration. On the gastric mucosa, the organism exists as a spiral form with one to seven sheathed flagella at one (usually) or both poles. Short spirals were seen in the first successful culture of the organism in 1983. In 1984, Marshall and Warren reported a coccoid form in older cultures. Since that time, other workers have observed rod and coccal forms in vitro; coccoid forms predominate in cultures 3-7 days old. We sought to examine the growth cycle of H. pylori in prolonged culture and the mode of coccoid body formation.

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