2,4-Dihydropyrazole glucosides 3a-3c were prepared and tested for theirantitumor activity. The structures of these compounds were established by 1H and 13C-NMR spectroscopy. Glucoside 3b shows an in vitro IC50 value of 16.4 μM againstproliferation of the human promyelotic leukemia (HL60) cell line.
1 August 2017 in European Journal of Medicinal Chemistry
4-Trifluoromethylpyridine derivatives 4–8 represent good candidates for the discovery of new antibacterial agents. Fluorinated pyridine nucleosides 4–7 and non-nucleoside analogues 8a,b were synthesized and evaluated for their antibacterial activities against Staphylococcus aureus, Bacillus infantis, Escherichia coli and Stenotrophomonas maltophilia. The minimum inhibitory concentrations (MICs) of the new nucleosides 4–7 range from 1.3 to 4.9 μg/mL and MICs of fluoroaryl derivatives 8a,b are in the range of 1.8–5.5 μg/mL. Activity of amoxicillin, the reference drug, is 1.0–2.0 μg/mL under similar conditions.
Two series of novel 3-cyano-2-(2′′,3′′,4′′-tri- O -acetyl- β - D -arabinopyranosyloxy)pyridones 5a–h and 9a,b were synthesized. Microwave irradiation has been used to obtain these products in high yield under milder conditions by the reaction of 2(1 H )-pyridone or its salt with an activated arabinose. The silyl method was used to obtain the same nuclesides 5a–h and 9a,b . Triethylamine was used to remove the acetyl protecting groups from the sugar moiety and to produce the free nucleosides 6a–h and 10a,b in 85–91% yield.
1 November 2017 in Bioorganic & Medicinal Chemistry Letters