Preparation and biological evaluation of metronidazole derivatives with monoterpenes and eugenol. (5th August 2018)

• Record Type: Journal Article
• Authors: Bkhaitan, Majdi M.; Alarjah, Mohammed; Mirza, Agha Zeeshan; Abdalla, Ashraf N.; El‐Said, Hamdi M.; Faidah, Hani S.
• Is Part Of: Chemical biology & drug design. Volume 92:Number 6(2018)
• Page Start: 1954
• Page End: 1962
• Publication Date: 2018-08-05
• Subjects: carvacrol -- Clostridium perfringens -- eugenol -- H. pylori -- menthol -- metronidazole -- monoterpenes -- thymol; Drugs -- Design -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; 615.19005
• DOI: 10.1111/cbdd.13366
• Languages: English
• ISSNs: 1747-0277

Abstract

Abstract: 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. Compound11 was highly active against all tested bacterial strains, especially against P12 with IC50 0.0011 μM/ml. Compound6 was highly active against C. perfringens with MIC 0.0094 nM/ml. Viability test was conducted for compound11 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. Abstract : 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 ).