Preparation and biological evaluation of metronidazole derivatives with monoterpenes and eugenol

Autor:	Mohammed Alarjah, Agha Zeeshan Mirza, Majdi M. Bkhaitan, Ashraf N. Abdalla, Hamdi M. El-Said, Hani S. Faidah
Rok vydání:	2018
Předmět:	Cell Survival Clostridium perfringens Microbial Sensitivity Tests medicine.disease_cause 01 natural sciences Biochemistry Cell Line chemistry.chemical_compound Acetic acid Clostridium Metronidazole Drug Discovery Eugenol medicine Humans Carvacrol Thymol Pharmacology Chromatography biology Helicobacter pylori 010405 organic chemistry Organic Chemistry Biological activity biology.organism_classification 0104 chemical sciences Anti-Bacterial Agents 010404 medicinal & biomolecular chemistry chemistry Monoterpenes Molecular Medicine medicine.drug
Zdroj:	Chemical biologydrug design. 92(6)
ISSN:	1747-0285
Popis:	Two series of metronidazole derivatives (ester derivatives and ether derivatives) were prepared reacting metronidazole and its acetic acid oxidized form with menthol, thymol, carvacrol, and eugenol. Both series of compounds were tested in vitro against two strains of Helicobacter pylori (the ATCC 26695 and P12), and one strain of Clostridium (Clostridium perfringens). Most of the prepared compounds showed biological activity against the targeted bacteria. Compound 11 was highly active against all tested bacterial strains, especially against P12 with IC50 0.0011 μM/ml. Compound 6 was highly active against C. perfringens with MIC 0.0094 nM/ml. Viability test was conducted for compound 11 to test its selectivity for normal human fetal lung fibroblasts (MRC5), and it was found to be non-toxic with IC50 more than 50 μM/ml.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::877840320a3a83da2fb83e1eaa195576 https://pubmed.ncbi.nlm.nih.gov/30022596 Zobrazit plný text záznamu Plný text ve formátu PDF Plný text ve formátu HTML
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