Germa-γ-lactones as novel inhibitors of bacterial urease activity

Amtul, Zareen; Follmer, Cristian; Mahboob, Sumera; Atta-ur-Rahman, _; Mazhar, Muhammad; Khan, Khalid Mohammed; Siddiqui, Rafat A.; Muhammad, Sajjad; Kazmi, Syed Jamil Hasan; Choudhary, M. Iqbal

doi:10.1016/j.bbrc.2007.02.158

Cited by 28 publications

(14 citation statements)

References 19 publications

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“…Although some of these compounds are potent urease inhibitors, their safety as well as their in vivo efficiency are yet to be determined 115 116. In addition, several compounds described in the literature display only a moderate inhibitory activity resulting in a low potential for clinical applications 77 117 118. Nevertheless, urease remains as one of the most important targets in the development of drugs for the management of gastric and urinary infections.…”

Section: Discussionmentioning

confidence: 99%

Ureases as a target for the treatment of gastric and urinary infections

2010

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Urease is known to be a major contributor to pathologies induced by Helicobacter pylori and Proteus species. In H pylori, urease allows the bacteria to survive in an acidic gastric environment during colonisation, playing an important role in the pathogenesis of gastric and peptic ulcers. Ureolytic activity also results in the production of ammonia in close proximity to the gastric epithelium, causing cell damage and inflammation. In the case of Proteus species (notably Proteus mirabilis) infection, stones are formed due to the presence of ammonia and carbon dioxide released by urease action. In addition, the ammonia released is able to damage the glycosaminoglycan layer, which protects the urothelial surface against bacterial infection. In this context, the administration of urease inhibitors may be an effective therapy for urease-dependent pathogenic bacteria. This is a review of the role of ureases in H pylori and Proteus species infections, focussing on the biochemical and clinical aspects of the most promising and/or potent urease inhibitors for the treatment of gastric and urinary tract infections.

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Section: Discussionmentioning

confidence: 99%

Ureases as a target for the treatment of gastric and urinary infections

2010

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“…The antibacterial activities of the complex against AMX-resistant clinical isolates (SA-6, 7, 17, 21, 31, and SA-34), CLT-resistant clinical isolates (SA-3, 4, 17, and SA-28), TET-resistant clinical isolates (SA-1, 3, 5, 14, and SA-21), and MNZ-resistant clinical isolates (SA-1, 3, 5-14, 16-22, and 6-34) were nearly comparable to those against AMX-, CLT-, TET-, and MNZ-susceptible isolates. The complex was also found to be equally effective against the strains showing double (SA- 1,6,7,21,28,31, and triple (SA-3, 5, and 17) drug resistance. With standard 7-14-day triple therapies, eradication of H. pylori is decreasing due to increased bacteria-resistant strains.…”

Section: Anti-h Pylori Activity (In Vitro)mentioning

confidence: 94%

Mechanochemical synthesis andin vitroanti-Helicobacter pyloriand uresase inhibitory activities of novel zinc(II)–famotidine complex

Amin

Iqbal

Hughes

et al. 2009

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…Amtul et al 68 demonstrated lactones as novel class of urease inhibitors. The synthesized GeL compounds were found to be highly selective in inhibiting the growth of Proteus mirabilis at moderate concentrations.…”

Section: Classes Of Urease Inhibitorsmentioning

confidence: 99%

Structurally Diversified Heterocycles and Related Privileged Scaffolds as Potential Urease Inhibitors: A Brief Overview

Ibrar

Khan

Abbas

2013

Archiv der Pharmazie

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Ureases have emerged as significant virulence factors implicated in the pathogenesis of many clinical conditions such as pyelonephritis, hepatic coma, peptic ulceration, and the formation of injection-induced urinary stones and stomach cancer. They have also been identified as important targets in research both for human and animal health, as well as in agriculture. Strategies based on urease inhibition are the main treatment of diseases caused by urease-producing bacteria. So, in the present context, a diverse library of chemical structures is known to possess remarkable inhibitory activities against urease enzymes. The current review article summarizes and discusses endeavours towards the developments in the burgeoning field of urease inhibition in medicinal chemistry, with an emphasis on the insights that have been gleaned into the structural features that contribute to high and promising levels of anti-urease activity.

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Germa-γ-lactones as novel inhibitors of bacterial urease activity

Cited by 28 publications

References 19 publications

Ureases as a target for the treatment of gastric and urinary infections

Ureases as a target for the treatment of gastric and urinary infections

Mechanochemical synthesis andin vitroanti-Helicobacter pyloriand uresase inhibitory activities of novel zinc(II)–famotidine complex

Structurally Diversified Heterocycles and Related Privileged Scaffolds as Potential Urease Inhibitors: A Brief Overview

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