3118-34-1Relevant academic research and scientific papers
Synthesis and antibiotic activity of novel acylated phloroglucinol compounds against methicillin-resistant Staphylococcus aureus
Mittal, Navriti,Tesfu, Haben H.,Hogan, Andrew M.,Cardona, Silvia T.,Sorensen, John L.
, p. 253 - 259 (2019/02/19)
The rise in antibiotic resistance among pathogenic microorganisms has created an imbalance in the drugs available for treatment, in part due to the slow development of new antibiotics. Cystic fibrosis (CF) patients are highly susceptible to antibiotic-resistant pathogens, including methicillin-resistant Staphylococcus aureus (MRSA). Phloroglucinols and related polyketide natural products have demonstrated antimicrobial activity against a number of Gram-positive bacteria including S. aureus. In this study, we investigated a series of acylated phloroglucinol derivatives to determine their potential as lead compounds for the design of novel therapeutics. To assess the activity of these compounds, we determined the minimum inhibitory and bactericidal concentration (MIC and MBC, respectively), the minimum biofilm inhibitory and biofilm eradication concentration (MBIC and MBEC, respectively), and evaluated hemolytic activity, as well as their interaction with clinically relevant antibiotics. Of the 12 compounds tested against MRSA and methicillin-susceptible strains, four showed MIC values ranging from 0.125 to 8 μg ml?1 and all of them were bactericidal. However, none of the compounds were able to eradicate biofilms at the concentrations tested. Three of the four did not display hemolytic activity under the conditions tested. Further studies on the interactions of these compounds with clinically relevant antibiotics showed that phlorodipropanophenone displayed synergistic activity when paired with doxycycline. Our results suggest that these acylated phloroglucinols have potential for being further investigated as antibacterial leads.
2. 4 - Diacetyl phloroglucinol analogue and its preparation method and application
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Paragraph 0024; 0031; 0050, (2018/05/30)
The invention discloses a 2,4-DAPG analogue and a preparation method and application thereof. The structure of the 2,4-DAPG analogue is shown as the formula (1) or formula (2), wherein R is C2-C15 alkyl, R1 and R2 are C1-C15 alkyl, and the R1 and the R2 a
Analogues of natural phloroglucinols as antagonists against both thromboxane A2 and leukotriene D4
Tada,Chiba,Takakuwa,Kojima
, p. 1209 - 1212 (2007/10/02)
Antagonists against both thromboxane A2 and leukotriene D4 were prepared from phloroglucinol. These compounds showed almost the same activity as the chinesins which were isolated from Hypericum chinense L. The correlation between the
Inhibitory effect of acylphloroglucinol derivatives on the replication of vesicular stomatitis virus.
Chiba,Takakuwa,Tada,Yoshii
, p. 1769 - 1772 (2007/10/02)
The antiviral activity of natural phloroglucinols and of synthesized mono- and diacylphloroglucinols, and 2,6-diacyl-4,4-dialkylcyclohexa-1,3,5-triones was investigated. A correlation between the acyl chain length and inhibitory activity against vesicular stomatitis virus (VSV) was observed. Potent antiviral activity was found in di-isovalerylphoroglucinol. 2,6-Diacyl-4,4-dialkylcyclohexa-1,3,5-triones inhibited replication of the virus with low cytotoxicity.
Structure/Activity relationships of Grandinol: a Germination Inhibitor in Eucalyptus
Bolte, Matthew L.,Crow, Wilfrid D.,Takahashi, Nobutaka,Sakurai, Akira,Uji-Ie, Masami,Yoshida, Shigeo
, p. 761 - 768 (2007/10/02)
Structure/activity relationships of grandinol (1), which shows potent inhibition to cress germination, were examined by an activity comparison of many synthetic analogues.The result clearly indicates that a combination of two carbonyl functionalities on a
