3098-40-6Relevant academic research and scientific papers
Selectivity, its anti-MRSA activity is about 50 myrtle ketone derivatives of vancomycin and its preparation method and use times.
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Paragraph 0063-0067, (2022/01/21)
A myrtle ketone derivative is a compound shown in formula (I), optical isomers, enantiomers, diastereomers, racemates and pharmaceutically acceptable salts thereof,
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
A natural product yellow filicic acid BB of full-synthesis method
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Paragraph 0009; 0019, (2019/01/08)
The invention relates to a natural product yellow filicic acid BB of full-synthesis method, which belongs to the technical field of organic chemistry. The invention from the economic and easy to synthesize the phloroglucinol proceed double-acylated phloroglucinol, then after iodine methane-to-carbon double methylation, removing monomolecular acyl got the midbody 3; to phloroglucinol as raw materials, acetate acylation to obtain the aldehyde phloroglucinol, reduction of the aldehyde is methyl, then acylated to obtain intermediate 6; the two fragments obtained through the Eschenmoser's salt combined yellow filicic acid BB. In the method 42% overall yield of yellow filicic acid improves the BB fully synthetic yield, raw material economy are easy, simple operation, high yield, and suitable for production, may be its biological activity study provide a large number of raw materials.
Dryopteris fragrans phloroglucinol compound flavaspidic acid BB and antibacterial application thereof
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Paragraph 0058; 0060; 0061, (2018/05/24)
The invention relates to the technical field of medicine and discloses an antibacterial application of a Dryopteris fragrans phloroglucinol compound flavaspidic acid BB. The invention provides the flavaspidic acid BB obtained by the chemical synthesis method. The flavaspidic acid BB has good antibacterial effects, effectively fills in the application deficiency of the antibacterial natural compound and provides an effective antibacterial solution for drug-resistant bacteria. The experimental results show that the compound has a strong antibacterial effect and good curative effects especially on drug-resistant bacteria.
Ortho-amidoalkylation of phenols via tandem one-pot approach involving oxazine intermediate
Mudududdla, Ramesh,Jain, Shreyans K.,Bharate, Jaideep B.,Gupta, Ajai P.,Singh, Baldev,Vishwakarma, Ram A.,Bharate, Sandip B.
, p. 8821 - 8827 (2012/11/07)
A new and efficient method for ortho-amidoalkylation of phenols via Mannich-type condensation with formaldehyde and lactams using recyclable solid acid catalyst is described. This is the first report for ortho-amidoalkylation of phenols by lactams via Mannich-type condensation. LC-ESI-MS/MS based mechanistic study revealed that reaction proceeds through o-quinone methide (o-QM) and an oxazine intermediate via tandem Knoevenagel condensation, formal [4 + 2]-Diels-Alder cycloaddition and acid catalyzed oxazine ring-opening.
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.
Phlorophenone derivatives, processes for preparing such compounds, uses and pharmaceutical compositions of phlorophenone compounds
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, (2008/06/13)
Novel compounds of general formula I STR1 wherein R is a branched or unbranched alkyl, cycloalkyl, or aralkyl group, which group optionally contains or is substituted by a halogen or oxygen function, the oxygen function optionally being in the form of an alcohol or ether moiety; R1, R2, and R3, which may be the same or different, is hydrogen, an alkyl, acyl, or benzoyl group, which group optionally contains or is substituted by a halogen or oxygen function; R4 is hydrogen, an alkyl, alkenyl preferably being an allyl or prenyl group, or aralkyl group which group optionally contains or is substituted by an alkyl, aryl, halogen or oxygen function; R5 is hydrogen, an alkyl, aralkyl, acyl, or aryl group, which group optionally contains or is substituted by an alkyl, aryl, halogen, or oxygen function; except that R4 and R5 are not both hydrogen; and except for the compounds when R5 is hydrogen and R is methyl, i-propyl, branched butyl, methoxy methyl, 2-phenylethyl, or 2-phenylethylene; chromans and dihydrobenzofurans derived from these compounds; pharmaceutically acceptable salts, and metabolites and metabolic precursors of these compounds; processes for preparing the aforementioned types of compounds; use of the aforementioned types of compounds as antibacterial and/or antimycotic agents; and pharmaceutical compositions of such compounds.
