{"title":"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。","authors":"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","doi":"10.1007/s11030-025-11306-3","DOIUrl":null,"url":null,"abstract":"<p><p>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.</p>","PeriodicalId":708,"journal":{"name":"Molecular Diversity","volume":" ","pages":""},"PeriodicalIF":3.8000,"publicationDate":"2025-07-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"A perspective on the synthetic methodologies and biological attributes of thiazole-hydrazone compounds: a medicinal chemistry-based investigation.\",\"authors\":\"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\",\"doi\":\"10.1007/s11030-025-11306-3\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>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.</p>\",\"PeriodicalId\":708,\"journal\":{\"name\":\"Molecular Diversity\",\"volume\":\" \",\"pages\":\"\"},\"PeriodicalIF\":3.8000,\"publicationDate\":\"2025-07-28\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Molecular Diversity\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://doi.org/10.1007/s11030-025-11306-3\",\"RegionNum\":2,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"CHEMISTRY, APPLIED\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Molecular Diversity","FirstCategoryId":"92","ListUrlMain":"https://doi.org/10.1007/s11030-025-11306-3","RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, APPLIED","Score":null,"Total":0}
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.
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;