- Natural products as sources of new fungicides (II): antiphytopathogenic activity of 2,4-dihydroxyphenyl ethanone derivatives
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A series of 17 simple 1-(2,4-dihydroxyphenyl) ethanones were synthesised, and their structures characterised by 1H, 13C NMR and ESI-MS. Their in vitro antifungal activities were evaluated against five phytopathogenic fungi including Glomerella cingulate, Botrytis cirerea, Fusarium graminearum, Curvularia lunata and Fusarium oxysporum f. sp. vasinfectum by the mycelial growth inhibition assay. Compounds 2g and 2h exhibited broad-spectrum inhibitory activity against the mycelial growth of the tested pathogens with IC50 values in the range of 16-36 g/mL, and in particular being more active to G. cingulate, with IC50 values of 16.50 and 19.25 g/mL, respectively, than the other pathogens. Preliminary SAR indicated that an α,β-unsaturated ketone unit of the alkyl chain of the compounds is the structure requirement for fungicidal action. The results suggested that 2g and 2h may be promising leads in the development of new antifungal agents.
- Nandinsuren, Tseden,Shi, Wei,Zhang, An-Ling,Bai, Yu-Bin,Gao, Jin-Ming
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supporting information
p. 1166 - 1169
(2016/04/20)
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- COMPOSITIONS AND METHODS OF USE OF ELECTRON TRANSPORT SYSTEM INHIBITORS
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The invention provides compounds of the formula: or a pharmaceutically acceptable salt thereof, where m, n, R1, R2, R3 R4, R5, R6, R7 are those defined herein. The invention also provides pharmaceutical compositions comprising a compound of the invention, methods for using compounds and/or pharmaceutical compositions of the invention, and methods for synthesizing compounds of the invention.
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- Discovery of 1,4-didydroxy-2-naphthoate prenyltransferase inhibitors: New drug leads for multidrug-resistant gram-positive pathogens
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Since utilization of menaquinone in the electron transport system is a characteristic of Gram-positive organisms, the 1,4-dihydroxy-2-naphthoate prenyltransferase (MenA) inhibitors 1a and 2a act as selective antibacterial agents against organisms such as methicillin-resistant Stapylococcus aureus (MRSA), Staphylococcus epidermidis (MRSE), and Mycobacterium spp. Growth of drug-resistant Gram-positive organisms was sensitive to the MenA inhibitors, indicating that menaquinone synthesis is a valid new drug target in Gram-positive organisms.
- Kurosu, Michio,Narayanasamy, Prabagaran,Biswas, Kallolmay,Dhiman, Rakesh,Crick, Dean C.
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p. 3973 - 3975
(2008/02/11)
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