One approach to overcome the antimicrobial resistance of many pathogens is to associate compounds with antimicrobial properties and obtain combinations superior compared to the effect of each compound. To identify a possible potentiating effect, we tested and analyzed the inhibitory effect of the combination of coumarin with two pyrazole derivatives, 1,1'-methandiylbis (3,5-dimethyl-1H-pyrazole (AM4) and 3,5-dimethyl-1H-pyrazol-1-yl) methanol 3,5-dimethyl-1-hydroxymethylpyrazol (SAM4). A clear synergistic effect was recorded when coumarin was associated with SAM4, in which case the Fractional Inhibitory Concentration Index (FICI) had a value equal to 0.468 for Citrobacter freundii, Proteus mirabilis, and E. coli. In the other cases, however, both the association between coumarin and AM4 and coumarin SAM4 had only an additive effect (FICI = 0.937-1.00). The bactericidal effect of the coumarin-pyrazole combination over time was better in all cases compared to the effect of the compounds used separately. The viability of the bacterial cells at sub-inhibitory concentrations of the tested compounds was variable, depending on both the type of compound and the bacterial strain.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1007/s00203-022-02773-5 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Coumarin derivatives as inhibitors of d-amino acid oxidase and monoamine oxidase.
Bioorg Chem
June 2022
Pharmaceutical Chemistry, School of Pharmacy and Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom 2520, South Africa. Electronic address:
d-Amino acid oxidase (DAAO) oxidises d-amino acids to ultimately produce the corresponding α-keto acids. The DAAO substrate, d-serine, is a co-agonist at NMDA receptors, while NMDA receptor hypo-function has been implicated in the pathophysiology of schizophrenia. Through the modulation of d-serine levels, the inhibition of DAAO represents a strategy to increase NMDA receptor function, and thus a potential treatment for schizophrenia.
View Article and Find Full Text PDFEffect of methylpyrazoles and coumarin association on the growth of Gram-negative bacteria.
Arch Microbiol
February 2022
Department of Natural Sciences, Faculty of Natural and Agricultural Sciences, Ovidius University of Constanta, 1, University Street, 900470, Constanta, Romania.
One approach to overcome the antimicrobial resistance of many pathogens is to associate compounds with antimicrobial properties and obtain combinations superior compared to the effect of each compound. To identify a possible potentiating effect, we tested and analyzed the inhibitory effect of the combination of coumarin with two pyrazole derivatives, 1,1'-methandiylbis (3,5-dimethyl-1H-pyrazole (AM4) and 3,5-dimethyl-1H-pyrazol-1-yl) methanol 3,5-dimethyl-1-hydroxymethylpyrazol (SAM4). A clear synergistic effect was recorded when coumarin was associated with SAM4, in which case the Fractional Inhibitory Concentration Index (FICI) had a value equal to 0.
View Article and Find Full Text PDFInvolvement of CYP2A6 in the formation of a novel metabolite, 3-hydroxypilocarpine, from pilocarpine in human liver microsomes.
Drug Metab Dispos
March 2007
Pharmacokinetics Research, Kissei Pharmaceutical Co., Ltd., 19-48 Yoshino Matsumoto-city, Nagano 399-8710, Japan.
Pilocarpine is a cholinergic agonist that is metabolized to pilocarpic acid by serum esterase. In this study, we discovered a novel metabolite in human urine after the oral administration of pilocarpine hydrochloride, and we investigated the metabolic enzyme responsible for the metabolite formation. The structure of the metabolite was identified as 3-hydroxypilocarpine by liquid chromatography-tandem mass spectrometry and NMR analyses and by comparing to the authentic metabolite.
View Article and Find Full Text PDFThe role of CYP2A and CYP2E1 in the metabolism of 3-methylindole in primary cultured porcine hepatocytes.
Drug Metab Dispos
May 2006
Department of Animal and Poultry Science, University of Guelph, Guelph, Ontario, Canada N1G 2W1.
The accumulation of 3-methylindole (3MI) in uncastrated male pigs (boars) is a major cause of boar taint, which negatively affects the quality of meat from the animal. Previously, CYP2E1 and CYP2A have been identified as cytochrome P450 (P450) isoforms involved in the metabolism of 3MI using porcine liver microsomes. This study further examines the role of these isoforms in the metabolism of 3MI using a primary porcine hepatocyte model by examining metabolic profiles of 3MI after incubation with P450 inhibitors.
View Article and Find Full Text PDFMetabolism of chloroform in the human liver and identification of the competent P450s.
Drug Metab Dispos
March 2003
Biochemical Toxicology Unit, Comparative Toxicology and Ecotoxicology Laboratory, Istituto Superiore di Sanità, Rome, Italy.
The oxidative and reductive cytochrome P450 (P450)-mediated chloroform bioactivation has been investigated in human liver microsomes (HLM), and the role of human P450s have been defined by integrating results from several experimental approaches: cDNA-expressed P450s, selective chemical inhibitors and specific antibodies, correlation studies in a panel of phenotyped HLM. HLM bioactivated CHCl(3) both oxidatively and reductively. Oxidative reaction was characterized by two components, suggesting multiple P450 involvement.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!