噻唑-腙类化合物的合成方法及生物学特性研究:基于药物化学的研究。

IF 3.8 2区 化学 Q2 CHEMISTRY, APPLIED
Pallishree Bhukta, Akash Verma, Roshan Kumar, Arockia Babu Marianesan, Suhas Ballal, Amrita Pal, Thakur Gurjeet Singh, Ganesh Bushi, Abhay M Gaidhane, Deepankar Rath, Prateek Pathak, Ashish Ranjan Dwivedi
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引用次数: 0

摘要

噻唑-腙类化合物结合了噻唑环和腙键的特点,是药物发现中必不可少的双杂环支架。由于每种成分的不同特性,这种组合提供了增强的生物活性和多功能性。噻唑环通过其硫原子和氮原子提供电子密度,有助于亲脂性和改善膜通透性,从而增强药物到达细胞内目标的能力。噻唑因其众多的生物学特性而被认可,包括抗癌、抗菌、抗炎,并在生物活动中用于神经和代谢紊乱,包括抗菌、抗癌和抗炎作用。同时,腙基团引入了与潜在的氢键给体和受体位点的柔性连接。它允许与生物靶标强烈的相互作用,使其成为靶向酶活性位点和受体口袋的理想选择。本文综述了这些多用途杂环化合物的最新进展及其在抗癌、抗炎、抗菌和抗结核治疗方面的药理活性。许多具有这种支架的化合物在治疗癌症和传染病方面的功效正在进行大量的临床试验。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
A perspective on the synthetic methodologies and biological attributes of thiazole-hydrazone compounds: a medicinal chemistry-based investigation.

Thiazole-hydrazone compounds serve as an essential bis-heterocyclic scaffold in drug discovery, combining the features of a thiazole ring and a hydrazone linkage. This combination offers enhanced biological activity and versatility due to the distinct characteristics of each component. The thiazole ring provides electron density through its sulfur and nitrogen atoms, contributing to lipophilicity and improved membrane permeability, which enhances the drug's ability to reach intracellular targets. Thiazoles are recognized for their numerous biological attributes encompassing anticancer, antibacterial, anti-inflammatory, and use for neurological and metabolic disorders in biological activities, including antimicrobial, anticancer, and anti-inflammatory effects. Meanwhile, the hydrazone group introduces a flexible linkage with potential hydrogen-bond donor and acceptor sites. It allows strong interactions with biological targets, making it ideal for targeting enzyme active sites and receptor pockets. The review article explores the recent developments in these versatile heterocyclic combinations and their promising pharmacological activity, particularly in anticancer, anti-inflammatory, antimicrobial, and anti-tubercular treatment. Many compounds featuring this scaffold are under investigation for their efficacy in treating cancer and infectious diseases in numerous clinical phase trials.

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来源期刊
Molecular Diversity
Molecular Diversity 化学-化学综合
CiteScore
7.30
自引率
7.90%
发文量
219
审稿时长
2.7 months
期刊介绍: Molecular Diversity is a new publication forum for the rapid publication of refereed papers dedicated to describing the development, application and theory of molecular diversity and combinatorial chemistry in basic and applied research and drug discovery. The journal publishes both short and full papers, perspectives, news and reviews dealing with all aspects of the generation of molecular diversity, application of diversity for screening against alternative targets of all types (biological, biophysical, technological), analysis of results obtained and their application in various scientific disciplines/approaches including: combinatorial chemistry and parallel synthesis; small molecule libraries; microwave synthesis; flow synthesis; fluorous synthesis; diversity oriented synthesis (DOS); nanoreactors; click chemistry; multiplex technologies; fragment- and ligand-based design; structure/function/SAR; computational chemistry and molecular design; chemoinformatics; screening techniques and screening interfaces; analytical and purification methods; robotics, automation and miniaturization; targeted libraries; display libraries; peptides and peptoids; proteins; oligonucleotides; carbohydrates; natural diversity; new methods of library formulation and deconvolution; directed evolution, origin of life and recombination; search techniques, landscapes, random chemistry and more;
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