124061-89-8Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of thiazole bioisosteres of goniofufurone through in vitro antiproliferative activity and in vivo toxicity
Djoki?, Sanja,Kesi?, Jelena,Koji?, Vesna,Pavi?, Aleksandar,Popsavin, Mirjana,Popsavin, Velimir,Rodi?, Marko V.,Sre?o Zelenovi?, Bojana,Svir?ev, Milo?,Vasiljevi?, Branka
, (2022/02/25)
The synthesis of several new goniofufurone bioisosteres was achieved in which the phenyl residue was replaced by a thiazole ring. The key steps of the synthesis included the initial condensation of cyanohydrin benzoates with cysteine ethyl ester hydrochlo
Glycosyl isoxazole compound, preparation method thereof and bactericide
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Paragraph 0122-0124; 0128; 0178-0179; 0182; 0185, (2021/04/07)
The invention relates to the technical field of bactericidal materials, and particularly relates to a glycosyl isoxazole compound, a preparation method thereof and a bactericide. The glycosyl isoxazole compound has a structural general formula shown in the description, wherein R1 is selected from any one of substituted or unsubstituted aromatic groups, and R2 is selected from any one of H, acetyl, benzyl and propargyl. According to the invention, a natural saccharide compound is adopted as the framework, the safety is provided, the toxicity is low, the selectivity is high, residue is not easily generated, the environmental compatibility is good, the active group isoxazole structure is further introduced, and the obtained glycosyl isoxazole compound has advantages of safety, high efficiency, low toxicity, low residue, broad spectrum, resistance generation resistance resistance resistance generation resistance and the like, and further has excellent bactericidal activity.
Tetrofuranose nucleoside phosphonic acids: Synthesis and properties
Polakova, Ivana,Budesinsky, Milos,Tocik, Zdenek,Rosenberg, Ivan
, p. 503 - 536 (2011/12/04)
New isoelectronic, non-isosteric phosphonate analogues of nucleoside 5'-phosphates featuring the phosphorus moiety directly attached on the sugar ring in the C4' position are described. The analogues were synthesised by a nucleosidation reaction from tetr
S-Ribosylhomocysteine analogues with the carbon-5 and sulfur atoms replaced by a vinyl or (fluoro)vinyl unit
Wnuk, Stanislaw F.,Lalama, Jennifer,Garmendia, Craig A.,Robert, Jenay,Zhu, Jinge,Pei, Dehua
, p. 5090 - 5102 (2008/12/21)
Treatment of the protected ribose or xylose 5-aldehyde with sulfonyl-stabilized fluorophosphonate gave (fluoro)vinyl sulfones. Stannyldesulfonylation followed by iododestannylation afforded 5,6-dideoxy-6-fluoro-6-iodo-d-ribo or xylo-hex-5-enofuranoses. Coupling of the hexenofuranoses with alkylzinc bromides gave 10-carbon ribosyl- and xylosylhomocysteine analogues incorporating a fluoroalkene. The fluoroalkenyl and alkenyl analogues were evaluated for inhibition of Bacillus subtilis S-ribosylhomocysteinase (LuxS). One of the compounds, 3,5,6-trideoxy-6-fluoro-d-erythro-hex-5-enofuranose, acted as a competitive inhibitor of moderate potency (KI = 96 μM).
