Design, Synthesis, and Biological Evaluation of Novel Pyrrolo [2,3-b] Pyridine Derivatives for Nonalcoholic Fatty Liver Disease

Nonalcoholic fatty liver disease (NAFLD) is featured with liver fat infiltration and accumulation with no connection with overdrinking. With the rising trends and no FDA-approved drugs, NAFLD attracts global attention. In this study, we successfully synthesized 18 novel SIS3 derivatives and evaluate...

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Main Authors: Jialin Ma, Jing Li, Dongping Yao, Qi Wang, Xinzhou Chen, Feiyan Tao, Bin Chen, Yongmei Xie, Lang Bai, Yiwen Zhang
Format: Article
Language:English
Published: Wiley 2022-01-01
Series:Journal of Chemistry
Online Access:http://dx.doi.org/10.1155/2022/2386212
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author Jialin Ma
Jing Li
Dongping Yao
Qi Wang
Xinzhou Chen
Feiyan Tao
Bin Chen
Yongmei Xie
Lang Bai
Yiwen Zhang
author_facet Jialin Ma
Jing Li
Dongping Yao
Qi Wang
Xinzhou Chen
Feiyan Tao
Bin Chen
Yongmei Xie
Lang Bai
Yiwen Zhang
author_sort Jialin Ma
collection DOAJ
description Nonalcoholic fatty liver disease (NAFLD) is featured with liver fat infiltration and accumulation with no connection with overdrinking. With the rising trends and no FDA-approved drugs, NAFLD attracts global attention. In this study, we successfully synthesized 18 novel SIS3 derivatives and evaluated them for pharmacological activity. F-9 and F-15 had potent weight-losing effects. Importantly, intraperitoneal administration of F-9 at 10 mg·kg−1·day−1 for 5 weeks had the most excellent effects to reduce the weight of the body, liver, and fat, as well as adjusting serum levels of AST, ALT, TC, TG, HDL, and LDL. H&E staining showed that F-9 could suppress fat deposition and increase the adipocyte size in the liver.
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institution Kabale University
issn 2090-9071
language English
publishDate 2022-01-01
publisher Wiley
record_format Article
series Journal of Chemistry
spelling doaj-art-965de418ea56463cb9ab696759b2b2922025-02-03T01:23:35ZengWileyJournal of Chemistry2090-90712022-01-01202210.1155/2022/2386212Design, Synthesis, and Biological Evaluation of Novel Pyrrolo [2,3-b] Pyridine Derivatives for Nonalcoholic Fatty Liver DiseaseJialin Ma0Jing Li1Dongping Yao2Qi Wang3Xinzhou Chen4Feiyan Tao5Bin Chen6Yongmei Xie7Lang Bai8Yiwen Zhang9Cancer CenterDepartment of NephrologyCancer CenterCancer CenterCancer CenterResearch and Development CentreCenter of Infectious DiseasesCancer CenterCenter of Infectious DiseasesCancer CenterNonalcoholic fatty liver disease (NAFLD) is featured with liver fat infiltration and accumulation with no connection with overdrinking. With the rising trends and no FDA-approved drugs, NAFLD attracts global attention. In this study, we successfully synthesized 18 novel SIS3 derivatives and evaluated them for pharmacological activity. F-9 and F-15 had potent weight-losing effects. Importantly, intraperitoneal administration of F-9 at 10 mg·kg−1·day−1 for 5 weeks had the most excellent effects to reduce the weight of the body, liver, and fat, as well as adjusting serum levels of AST, ALT, TC, TG, HDL, and LDL. H&E staining showed that F-9 could suppress fat deposition and increase the adipocyte size in the liver.http://dx.doi.org/10.1155/2022/2386212
spellingShingle Jialin Ma
Jing Li
Dongping Yao
Qi Wang
Xinzhou Chen
Feiyan Tao
Bin Chen
Yongmei Xie
Lang Bai
Yiwen Zhang
Design, Synthesis, and Biological Evaluation of Novel Pyrrolo [2,3-b] Pyridine Derivatives for Nonalcoholic Fatty Liver Disease
Journal of Chemistry
title Design, Synthesis, and Biological Evaluation of Novel Pyrrolo [2,3-b] Pyridine Derivatives for Nonalcoholic Fatty Liver Disease
title_full Design, Synthesis, and Biological Evaluation of Novel Pyrrolo [2,3-b] Pyridine Derivatives for Nonalcoholic Fatty Liver Disease
title_fullStr Design, Synthesis, and Biological Evaluation of Novel Pyrrolo [2,3-b] Pyridine Derivatives for Nonalcoholic Fatty Liver Disease
title_full_unstemmed Design, Synthesis, and Biological Evaluation of Novel Pyrrolo [2,3-b] Pyridine Derivatives for Nonalcoholic Fatty Liver Disease
title_short Design, Synthesis, and Biological Evaluation of Novel Pyrrolo [2,3-b] Pyridine Derivatives for Nonalcoholic Fatty Liver Disease
title_sort design synthesis and biological evaluation of novel pyrrolo 2 3 b pyridine derivatives for nonalcoholic fatty liver disease
url http://dx.doi.org/10.1155/2022/2386212
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