2022
DOI: 10.3390/molecules27030931
|View full text |Cite
|
Sign up to set email alerts
|

Discovery of Novel Pleuromutilin Derivatives as Potent Antibacterial Agents for the Treatment of MRSA Infection

Abstract: A series of novel pleuromutilin derivatives containing nitrogen groups on the side chain of C14 were synthesized under mild conditions. Most of the synthesized derivatives displayed potent antibacterial activities. Compound 9 was found to be the most active antibacterial derivative against MRSA (MIC = 0.06 μg/mL). Furthermore, the result of time-kill curves showed that compound 9 had a certain inhibitory effect against MRSA in vitro. Moreover, according to a surface plasmon resonance (SPR) study, compound 9 (K… Show more

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...
2
1
1

Citation Types

0
5
0

Year Published

2022
2022
2024
2024

Publication Types

Select...
6

Relationship

0
6

Authors

Journals

citations
Cited by 6 publications
(5 citation statements)
references
References 41 publications
0
5
0
Order By: Relevance
“…It should be noted that results obtained with microsomes cannot be used for quantitative estimations of in vivo biotransformation [ 71 ]. As TIA was reported to have a high inhibitory effect on CYP3A4 in human liver microsomes with an IC 50 of 1.6 μM [ 69 ], data obtained in the present study exhibited that the pharmacokinetic parameters, such as AUC but not V d , CL, MRT, of AFB1 were altered after oral co-administration with TIA in chicken.…”
Section: Discussionmentioning
confidence: 46%
See 1 more Smart Citation
“…It should be noted that results obtained with microsomes cannot be used for quantitative estimations of in vivo biotransformation [ 71 ]. As TIA was reported to have a high inhibitory effect on CYP3A4 in human liver microsomes with an IC 50 of 1.6 μM [ 69 ], data obtained in the present study exhibited that the pharmacokinetic parameters, such as AUC but not V d , CL, MRT, of AFB1 were altered after oral co-administration with TIA in chicken.…”
Section: Discussionmentioning
confidence: 46%
“…Pleuromutilin derivatives like TIA can inhibit CYP3A4 activity with an IC 50 of 1.6 μM and showed strong inhibition to CYP450 enzymes [ 69 ]. In contrast, the IC 50 values for CYP2A6 and CYP2E1 were 7.6 μM and 47.6 μM in CLM in this study, respectively.…”
Section: Discussionmentioning
confidence: 99%
“…Pleuromutilin and its derivatives such as valnemulin, tiamulin, azamulin, and retapamulin have also shown significant antibacterial agents against MRSA. The probable mechanism might be the inhibition of protein synthesis by binding with peptidyl transferase constituents of 50S-subunit of ribosomes of bacteria [35]. Phloroglucinol and its acylphloroglucinol derivatives have shown promising anti-MRSA action.…”
Section: Natural Productsmentioning
confidence: 99%
“…The natural product pleuromutilin ( 1 , Figure ), discovered in 1951, , is an attractive foundation for new antibiotics. This is emphasized by the more than 40 pleuromutilin medicinal chemistry and total synthesis articles published within the field over the last 5 years, with some reporting very potent activity and high clinical potential, and in some cases also by employing novel and unique strategies. ,,,,, …”
Section: Introductionmentioning
confidence: 99%