| Summary: | 碩士 === 中原大學 === 化學研究所 === 101 === Glycolipid compounds GPS-1 (18), GS (18), and GO (18) synthesized in our laboratory , we found that GPS-3 (18) than the other two high GS (18) and GO (18). After comparing the three structural differences, we GPS-1 (18) is the lead compound (lead compound), Synthesized a series ofsaturated fatty acids with differrent carbon number of glycolipid compoundsGPS-1 series, explore a systematic relationship between the structure andbiological activity (structure-acti-
vety relationship, SAR).
GPS-1 series of compounds is N-acetyl glucosamine (glucosamine) as a starting material, via a plurality of oxide acetylation (per-O-acetylation), cyclization reaction (cyclization), glycosylation reaction (glycosylation)
, N-tertiary-butoxycarbonyl-amidation reaction (amidization) and the hydrogenation reaction (hydrogenation) and other five steps to prepare the compound GS-5.Compound GS-5 and then with FMOC-L-proline
(Fmoc-L-Proline) conductedamidation reaction (amidization), then de 9-fluorenyl methoxycarbonyl(fluorenylmethyloxycarbonyl, Fmoc) reacts with different unsaturated carboxylic acid amide having a carbon number of the amination reaction, and thedeacetylation reaction to tert-butoxycarbonyl
(t-butyloxycarbonyl, Boc) reaction, the five-step reaction to obtain the target GPS-1.
Activity test parts: for a single dose (10 μM) of the activity test, we found
thispart of a series of compounds has a significant inhibitory effect, but some
with no apparent biological significance, and not because of the length of the carbon chain showed a correlation , visibility, influence the activity of the carbon chain is not the main reason. In addition, we have also done a multiple dose (10,20,30 μM) activity test and found that this series of compounds at concentrationsincrease, the correct time will increase its
inhibitory activity.
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