THE SYNTHESIS AND GLYCOSIDASE INHIBITORY ACTIVITY OF ANALOGUES OF TIRUCHANDURAMINE
THE SYNTHESIS AND GLYCOSIDASE INHIBITORY ACTIVITY OF ANALOGUES OF TIRUCHANDURAMINE
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DOI：
10.3987/com-20-14236
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发表时间：
2020-04-01
期刊：
影响因子：
0.6
通讯作者：
Murphy, Patrick J.
中科院分区：
文献类型：
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作者：
Ashworth, Zackary J. R.;Bartholomew, Barbara;Murphy, Patrick J.
制备了代谢产物替鲁钱度胺1的5种类似物（7a-e）。化合物7 d和7 e是酵母α-葡萄糖苷酶的特异性抑制剂，而7 e特异性抑制芽孢杆菌α-葡萄糖苷酶。化合物7 b和7 c是最好的β-葡萄糖苷酶抑制剂。所有5种化合物都抑制β-半乳糖苷酶，但7 e再次是最好的抑制剂。显然，化合物7a-e中的不同链长影响抑制程度。与替鲁钱度胺1相比，一些合成类似物显示出对α-葡糖苷酶的显著改善的抑制，并且还显示出改善的特异性。
Five analogues (7a-e) of the metabolite tiruchanduramine 1 were prepared. Compounds 7d and 7e were specific inhibitors of yeast alpha-glucosidase, whilst 7e specifically inhibited Bacillus alpha-glucosidase. Compounds 7b and 7c were the best inhibitors of beta-glucosidase. All 5 compounds inhibited beta-galactosidase, but once again 7e was the best inhibitor. It was apparent that different chain lengths in the compounds 7a-e affect the degree of inhibition. Some of the synthetic analogues show significantly improved inhibition of alpha-glucosidases when compared to tiruchanduramine 1 and also improved specificity.