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方便地合成并研究了苯并噻唑连接的羟吡唑啉酮类化合物，这些化合物靶向α-淀粉酶和α-葡萄糖苷酶。

Facile synthesis and studies of benzothiazole-linked hydroxypyrazolones targeting -amylase and -glucosidase.

机构信息

Department of Chemistry, Guru Jambheshwar University of Science & Technology, Hisar, Haryana, 125001, India.

Department of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, Shoolini University, Solan, 173229, India.

出版信息

Future Med Chem. 2024;16(10):999-1027. doi: 10.4155/fmc-2023-0384. Epub 2024 May 22.

DOI:10.4155/fmc-2023-0384
PMID:38910576
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11221549/
Abstract

The objective of the present investigation was to design and synthesize new heterocyclic hybrids comprising benzothiazole and indenopyrazolone pharmacophoric units in a single molecular framework targeting α-amylase and α-glucosidase enzymatic inhibition. 20 new benzothiazole-appended indenopyrazoles, , were synthesized in good yields under environment-friendly conditions via cycloaddition reaction, and assessed for antidiabetic activity against α-amylase and α-glucosidase, using acarbose as the standard reference. Among all the hydroxypyrazolones, and showed the best inhibition against α-amylase and α-glucosidase, which finds support from molecular docking and dynamic studies. Compounds and have been identified as promising antidiabetic agents against α-amylase and α-glucosidase and could be considered valuable leads for further optimization of antidiabetic agents.

摘要

本研究旨在设计和合成新型杂环杂合体，这些杂合体包含苯并噻唑和茚并吡唑酮药效团单元，在单一分子框架内靶向α-淀粉酶和α-葡萄糖苷酶的抑制。通过加成反应，在环境友好条件下以良好的产率合成了 20 种新的苯并噻唑取代的茚并吡唑， ，并评估了它们对α-淀粉酶和α-葡萄糖苷酶的抗糖尿病活性，以阿卡波糖作为标准参考。在所有的羟基吡唑啉酮中， 和 对α-淀粉酶和α-葡萄糖苷酶的抑制作用最好，这一结果得到了分子对接和动力学研究的支持。化合物 和 已被确定为有希望的抗α-淀粉酶和α-葡萄糖苷酶的抗糖尿病药物，它们可以被认为是进一步优化抗糖尿病药物的有价值的先导化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bfd6/11221549/b573a9ef23fa/IFMC_A_2340244_UF0001_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bfd6/11221549/b573a9ef23fa/IFMC_A_2340244_UF0001_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bfd6/11221549/b573a9ef23fa/IFMC_A_2340244_UF0001_C.jpg

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Facile synthesis and studies of benzothiazole-linked hydroxypyrazolones targeting -amylase and -glucosidase.

Future Med Chem. 2024

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本文引用的文献

[1]
Recent advances in the synthesis of new benzothiazole based anti-tubercular compounds.

RSC Adv. 2023-7-21

[2]
Pyrazole; A Privileged Scaffold of Medicinal Chemistry: A Comprehensive Review.

Curr Top Med Chem. 2023

[3]
Global, regional, and national burden of diabetes from 1990 to 2021, with projections of prevalence to 2050: a systematic analysis for the Global Burden of Disease Study 2021.

Lancet. 2023-7-15

[4]
Novel Benzothiazole Derivatives as Potential Anti-Quorum Sensing Agents for Managing Plant Bacterial Diseases: Synthesis, Antibacterial Activity Assessment, and SAR Study.

J Agric Food Chem. 2023-5-3

[5]
Review on the Developments of Benzothiazole-containing Antimicrobial Agents.

Curr Top Med Chem. 2022

[6]
Pyrazole-containing pharmaceuticals: target, pharmacological activity, and their SAR studies.

RSC Med Chem. 2022-8-26

[7]
Synthesis, characterization, in-silico, and pharmacological evaluation of new 2-amino-6‑trifluoromethoxy benzothiazole derivatives.

Bioorg Chem. 2023-1

[8]
Vicinal Diaryl-Substituted Isoxazole and Pyrazole Derivatives with Growth Inhibitory and Antitumor Activity.

ACS Omega. 2022-10-3

[9]
A close look into the biological and synthetic aspects of fused pyrazole derivatives.

Eur J Med Chem. 2022-12-5

[10]
N-glycosylation induced changes in tau protein dynamics reveal its role in tau misfolding and aggregation: A microsecond long molecular dynamics study.

Proteins. 2023-2

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