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Design, synthesis and evaluation of l -quebrachitol derivatives against α-glycosidase

Two series of l -quebrachitol derivatives have been designed and synthesized in order to search for novel hypoglycemic agents. The α-glycosidase inhibitory activities of these compounds were evaluated, and their structure–activity relationships (SARs) were discussed. Using Acarbose as the positive c...

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Published in:New journal of chemistry 2023-07, Vol.47 (28), p.13387-13396
Main Authors: Zhang, Maoying, Liang, Xinjie, Cai, Pengcheng, Feng, Qixun, Chen, Yongsong, Yu, Xiaoxi, Zhang, Kuo, Bao, Xuefei, Chen, Guoliang
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container_end_page 13396
container_issue 28
container_start_page 13387
container_title New journal of chemistry
container_volume 47
creator Zhang, Maoying
Liang, Xinjie
Cai, Pengcheng
Feng, Qixun
Chen, Yongsong
Yu, Xiaoxi
Zhang, Kuo
Bao, Xuefei
Chen, Guoliang
description Two series of l -quebrachitol derivatives have been designed and synthesized in order to search for novel hypoglycemic agents. The α-glycosidase inhibitory activities of these compounds were evaluated, and their structure–activity relationships (SARs) were discussed. Using Acarbose as the positive control, the activities of 16 synthesized compounds against α-glycosidase were evaluated with 4-nitrophenyl-α- d -glucopyranoside as a substrate. The results showed that 16 compounds had significant inhibitory activities against α-glycosidase and 8 compounds (6b, 3b, 3c, 3e, 3h, 3i, 3j, and 3l) out of them had stronger inhibitory activities than Acarbose. Furthermore, 3i has the strongest activity, which is 20 times stronger than that of Acarbose.
doi_str_mv 10.1039/D3NJ00889D
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source Royal Society of Chemistry:Jisc Collections:Royal Society of Chemistry Read and Publish 2022-2024 (reading list)
subjects Glycosidases
Quebrachitol
Substrates
Synthesis
title Design, synthesis and evaluation of l -quebrachitol derivatives against α-glycosidase
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