203258-44-0Relevant articles and documents
Modification of Biphenolic Anti-Bacterial to Achieve Broad-Spectrum Activity
Kozlowski, Marisa C.,Ochoa, Cristian,Roenfanz, Hanna F.
, (2022/02/25)
The Gram-positive bacteria, methicillin-resistant Staphylococcus aureus (MRSA) and Gram-negative bacteria, Acinetobacter baumannii, are pathogens responsible for millions of nosocomial infections worldwide. Due to the threat of bacteria evolving resistance to antibiotics, scientists are constantly looking for new classes of compounds to treat infectious diseases. The biphenolic analogs of honokiol that were most potent against oral bacteria had similar bioactivity against MRSA. However, all the compounds proved ineffective against A. baumannii. The inability to inhibit A. baumannii is due to the difficult-to-penetrate lipopolysaccharide-coated outer membrane that makes it challenging for antibiotics to enter Gram-negative bacteria. The C 2 scaffold was optimized from the inhibition of Gram-positive bacteria to broad-spectrum antibacterial compounds that inhibit the dangerous Gram-negative pathogen A. baumannii.
The synthesis and glycosidase inhibitory activity of analogues of tiruchanduramine
Ashworth, Zackary J. R.,Bartholomew, Barbara,Evans, Daniel M.,Forde-Thomas, Josephine,Hoffmann, Karl F.,Murdoch, Reece,Murphy, Patrick J.,Nash, Robert J.,Sharp, Hazel,Whiteland, Helen
, p. 609 - 621 (2020/06/01)
Five analogues (7a-e) of the metabolite tiruchanduramine 1 were prepared. Compounds 7d and 7e were specific inhibitors of yeast α-glucosidase, whilst 7e specifically inhibited Bacillus α-glucosidase. Compounds 7b and 7c were the best inhibitors of β-gluco
Dimeric indole alkaloid compounds, preparation method thereof and use thereof in preparation of antibacterial drugs
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Paragraph 0036; 0037, (2019/04/30)
The present invention belongs to the fields of organic synthesis and pharmaceutical chemistry. In particular, the present invention relates to a series of dimeric indole alkaloid compounds as shown instructural general formula I, a preparation method thereof and use thereof in preparation of antibacterial drugs. After in vitro activity screening, results show that the compounds have strong antibacterial activity, in particular have specific inhibitory effects on strains of gram-positive bacteria such as staphylococcus, bacillus and enterococcus, and related drug-resistant strains thereof, andcan be used as lead compounds for developing new antibacterial drugs.