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Resolution and evaluation of 3-chlorophenyl-3-hydroxypropionylhydroxamic acid as antivirulence agent with excellent eradication efficacy in Helicobacter pylori infected mice by Liu, Qi; Ni, Wei-Wei; Li, Zhen; Bai, Cai-Fu; Tan, Dan-Dan; Pu, Chang-Jun; Zhou, Dong; Tian, Qing-Peng; Luo, Ni; Tan, Kai-Li; Dai, Le; Yan, Yuan; Pei, Yong; Li, Xian-Hui; Zhu, Hai-Liang; Xiao, Zhu-Ping is a Pharmacology, Toxicology and Pharmaceutics article available to read on EtoBox.
What is Resolution and evaluation of 3-chlorophenyl-3-hydroxypropionylhydroxamic acid as antivirulence agent with excellent eradication efficacy in Helicobacter pylori infected mice about?
The continuing emergence of drug-resistant Helicobacter pylori (HP) drives the ongoing need for the development of new and effective anti-HP drugs. Urease inhibitor has now gained strong interest as an alternative approach for HP infections. 3-Chlorophenyl-3-hydroxypropionylhydroxamic acid (CPH), a novel urease inhibitor identified in our group, shows impressive potency, which was optically separated for a further exploration. Here, we report in vitro/in vivo pharmacological evaluation of (±)-CPHs and the enantiomers. The raceme and the individual enantiomers significantly suppress gastritis at 32 mg/kg b.i.d dose with lower toxicity to mammalian cells (with CCs ≥ 3.16 mM) and mice (LDs ≥ 2338 mg/kg) than the clinically used agent acetohydroxamic acid. Furthermore, a significant increase of eradication of HP is observed for the combination of (±)-CPHs or the enantiomers with an antimicrobial. These studies revealed that CPH is a promising candidate for an alternative treatment of HP-dependent conditions by targeting virulence factor urease, and CPH may be used as a raceme.
Who reads Resolution and evaluation of 3-chlorophenyl-3-hydroxypropionylhydroxamic acid as antivirulence agent with excellent eradication efficacy in Helicobacter pylori infected mice?
It is typically read by researchers, students, and practitioners in Pharmacology, Toxicology and Pharmaceutics.
- Author
- Liu, Qi; Ni, Wei-Wei; Li, Zhen; Bai, Cai-Fu; Tan, Dan-Dan; Pu, Chang-Jun; Zhou, Dong; Tian, Qing-Peng; Luo, Ni; Tan, Kai-Li; Dai, Le; Yan, Yuan; Pei, Yong; Li, Xian-Hui; Zhu, Hai-Liang; Xiao, Zhu-Ping
- Publisher
- Elsevier Science; Elsevier ; Elsevier BV (ISSN 0928-0987)
- Published
- 2018
- Language
- EN
- Field
- Pharmacology, Toxicology and Pharmaceutics (Life Sciences)