氨基噻唑类化合物的合成研究进展

氨基噻唑化合物是重要的N-杂环化合物,近年来被广泛应用于工业生产、药物研发等多个领域,因此氨基噻唑类化合物的合成受到了越来越多的关注.对氨基噻唑类化合物的新型催化体系及新型方法进行了综述.     

噻唑并嘧啶类化合物的合成研究进展

综述了在医药和农药领域具有广泛用途的噻唑并嘧啶类化合物近二十年来合成方法上的研究进展. 结合本研究组在这一领域的工作介绍了噻唑并嘧啶类化合物的三种主要结构类型: 噻唑并[3,2-a]嘧啶、噻唑并[4,5-d]嘧啶、噻唑并[5,4-d]嘧啶类化合物的相关合成方法及新进展.     

2-咪唑啉类化合物的合成及应用研究新进展

2-咪唑啉是一类重要的五元含氮杂环化合物,基于其良好的反应性及生物活性在药物化学、天然产物化学、防腐缓蚀及催化等领域应用广泛,一直以来此类化合物的合成和应用拓展倍受关注.综述了近年来2-咪唑啉类化合物合成及其应用研究的新进展.     

苝类化合物研究与应用

苝类化合物具有大的共轭体系,易于进行结构修饰,可引入各种功能性基团,这种奇特结构赋予了苝类化合物优良的理化性质和特殊功能,在材料科学、超分子化学、生物、药学、医学等领域具有宽广的应用潜力,尤其在苝类有机光电材料已得到广泛的研究,取得了许多重要成就。尤其是近来越来越多的研究致力于开发苝类化合物其它可能的应用,已延伸到诸多领域,特别是相关生物医药的应用研究已成为近几年来异常活跃的新兴研究领域,引起广泛关注,进展迅速。本文结合课题组的研究工作,参考国内外近五年文献,首次系统地综述了苝类化合物在有机光电材料、纳米材料、生物医药光敏剂、生物荧光标记和成像、药物载体、人工诊断剂、人工离子受体和荧光分子探针等材料、生物、医药领域应用研究新进展。文中注重强化了化合物结构对苝类化合物性质和应用的影响。对未来苝类化合物研究与应用的发展趋势作了展望。     

基于烯基叠氮合成含氮杂环化合物的研究进展

自1910年首次被报道以来,烯基叠氮类化合物受到了化学工作者们广泛的关注.作为一类重要的有机合成中间体,尤其是在过渡金属催化下合成氮杂环类化合物方面,烯基叠氮类化合物有着广泛的应用.主要综述了烯基叠氮类化合物在构建含氮杂环化合物领域的研究进展.     

合成2,5-二芳基噻唑衍生物的新方法

噻唑环作为一类重要的五元芳香杂环,其衍生物具有多种生物活性,被广泛应用在医药方面.以价廉易得的不同取代苯甲酸为原料,经酰化反应、硫代反应、环合反应和Heck反应合成了2,5-二芳基噻唑衍生物.重点在于优化Heck反应的条件,进行可能反应机理的探讨.该方法具有反应条件温和、操作简单及底物的普适性良好等优点,为2,5-二芳基取代噻唑类化合物的合成提供了新的方向.     

四唑类化合物的合成及应用研究新进展

四唑是一种重要的五元芳杂环,具有多氮富电子的平面结构特征.这种特殊的结构使得四唑类化合物作为药物、炸药、功能材料等在医学、农学、材料科学等众多领域具有广泛的应用前景.相关研究十分活跃,已取得了许多重要进展.结合作者唑类方面的研究,参考国内外近五年文献,系统地综述了四唑类化合物的合成及其在医药、农药、材料等领域的应用研究新近况.     

酰胺类化合物的高效合成研究

酰胺类化合物是有机化学中最常见的化合物之一, 在药物化学、生物化学以及高分子合成等领域都有着重要的应用. 近年来高效合成酰胺类化合物已经成为一个研究热点, 具有重要的意义.本文主要从过渡金属催化、有机小分子催化等方面讨论近几年来酰胺类化合物的合成研究进展, 并对其发展趋势进行展望.     

富氮唑环类化合物的环加成合成研究进展

富氮唑环类化合物作为一种重要的氮杂环化合物,在药物化学、生物耦合、材料化学等领域有广阔的应用前景,其环加成合成的研究也越来越受人们的关注.从催化体系类型、合成不同取代类型产物等方面对近年来富氮唑环类化合物环加成合成方法的研究进展进行综述.     

二苯乙烯类化合物合成方法研究进展

二苯乙烯类化合物是具有1,2-二苯乙烯骨架结构的一类化合物.该类化合物在化学、医药、电子、光学及材料科学等领域具有广泛的应用,其化学合成方法引起了国内外研究人员的高度重视.本文结合作者和国内外学者对这方面的相关研究,对二苯乙烯类化合物的合成方法研究进展进行综述.     

芴类化合物的研究新进展

芴及其衍生物是一类重要的具有刚性平面联苯结构的化合物,分子内含有较大的共轭体系,这种特殊的刚性稠环结构使芴类化合物表现出许多独特的光电性能及生物活性,在光电材料、医药等多领域具有潜在的广泛应用.更为重要的是芴类化合物易于进行结构修饰,在芴环上可方便地引入各种功能基,芴类衍生物的合成及其开拓芴类化合物潜在的新用途,成为近些年来十分活跃的研究领域,且发展迅速.结合自己的工作,参考国内外文献,全面综述了芴类化合物在有机电致发光材料、双光子吸收材料、光致变色材料、太阳能电池材料和生物医药等领域的研究与开发新进展,并对其发展趋势作了展望.     

三唑类超分子化学与药物研究新进展

三唑环为含有三个氮原子的五元杂环, 唑环具有芳香性和丰富的电子, 易接受质子和络合金属离子, 因而三唑类化合物易通过配位键、氢键、离子-偶极、阳离子-?、?-?堆积、疏水效应以及范德华力等非共价键力形成超分子聚集体, 表现出许多特殊的性能及生物活性, 具有广泛的潜在应用如作为离子受体、材料、医药等. 近些年来, 相关三唑类超分子化学与医药的研究非常活跃, 发展特别迅速, 已成为十分活跃的热点研究领域. 本文结合自己的工作, 参考国内外近五年文献, 首次系统综述了三唑类化合物作为阳离子和阴离子受体以及三唑类超分子作为发光与磁性材料、医药在抗菌、抗真菌、抗癌等方面的研究与开发近况. 希望本综述对三唑类超分子化学与药物的进一步研发有所启迪.     

Overview on the recently developed thiazolyl heterocycles as useful therapeutic agents

Thiazoles are important heterocyclic compounds which have many biological activities and different applications such as useful ligands, in optical sensors, etc. A literature survey shows that there are different routes to thiazoles. One of the most frequently used synthetic approaches consists of a reaction between α-halocarbonyl compounds with a CSNH₂ moiety. In this mini-review we have classified the contents based on the reagent or material providing the sulfur atom of the thiazole ring. Also, among many articles which have been devoted to thiazole syntheses here we presented some synthetic approaches published from 2012 to 2014.     

Thiazole Ring—A Biologically Active Scaffold

Background: Thiazole is a good pharmacophore nucleus due to its various pharmaceutical applications. Its derivatives have a wide range of biological activities such as antioxidant, analgesic, and antimicrobial including antibacterial, antifungal, antimalarial, anticancer, antiallergic, antihypertensive, anti-inflammatory, and antipsychotic. Indeed, the thiazole scaffold is contained in more than 18 FDA-approved drugs as well as in numerous experimental drugs. Objective: To summarize recent literature on the biological activities of thiazole ring-containing compounds Methods: A literature survey regarding the topics from the year 2015 up to now was carried out. Older publications were not included, since they were previously analyzed in available peer reviews. Results: Nearly 124 research articles were found, critically analyzed, and arranged regarding the synthesis and biological activities of thiazoles derivatives in the last 5 years.     

Synthesis of Ethyl 8‐Aryl‐8‐hydroxy‐3‐oxo‐8H[1,2,4]oxadiazolo‐[3,4‐c][1,4]thiazine‐5‐carboxylates by Ring‐Expansion Rearrangement

The title compounds were prepared by the ring–ring interconversion of ethyl 5‐nitroso‐6‐arylimidazo[2,1‐b]thiazole‐3‐carboxylates with hydrochloric acid. The effect of electron‐withdrawing substituent in the thiazole ring on the general applicability of the ring–ring interconversion has been also evaluated.     

Metal complexes of biological active 2-aminothiazole derived ligands

The most imperative outcomes of extensive sterdies (synthesis, spectral, structural characterization and biological applications) of metal complexes with thiazole derived ligands are reviewed. A large number of coordination compounds are known but still there is a need of new compounds to develop various efforts in different fields for biomedical applications. The synthesis of Schiff base ligands is very important, and it has recently drawn the attention of numerous research groups, making this area constantly evolve. Authors are also synthesizing some novel biologically potent ligands and their unique complexes and complexes found more biological active agents than that of ligands against bacteria, fungi and herbs. Highlights: Schiff bases and their metal chelates catalyze reactions; Schiff bases derived from sulfane thiadiazole show toxicities against insects; Schiff bases of thiadiazole have good plant regulator activity; Phenyl ring attached to the thiazole group showed interesting structure activity.     

New Derivatives of Thiazole with Mesomorphous Properties

Azomethines containing a thiazole ring have been synthesized and their liquid crystal properties have been investigated. The influence of the central group and substituents in the azomethine component on the type and temperature range of the mesomorphous properties of the compounds synthesized has been elucidated.     

Mass spectra of derivatives of imidazo[2,1-b] thiazole and thiazolo[3,2-a]benzimidazole

The mass spectra of 6-phenylimidazo[2,1-b]thiazole, thiazolo[3,2-a]benzimidazole, and a number of thiazole-ring-substituted derivatives were investigated. The fragmentation of both groups of compounds commences with cleavage of the bonds in the thiazole ring and leads to the appearance of nitrogen- and sulfur-containing fragments in the spectra. The common character of the mass spectrometric disintegration of the investigated compounds indicates that they have similar electronic structures. The mass number and position of a substituent in the thiazole ring can be determined on the basis of the mass numbers of a series of fragments.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 6, pp. 778–783, June, 1974.     

Syntheses of aromatic substituted hydrazino-thiazole derivatives to clarify structural characterization and antioxidant activity between 3-arylsydnonyl and aryl substituted hydrazino-thiazoles

This work clarifies the structural characterization and antioxidant activity between aromatic and 3-arylsydnonyl substituted hydrazino-thiazoles by further synthesizing a series of aromatic ring-substituted hydrazino-thiazole derivatives 8a-h and 9a-h. Hydrazino-thiazole derivatives 8a-h and 9a-h were obtained by reacting aromatic or heterocyclic aromatic aldehyde thiosemicarbazones 7a-h with cyclization reagents ethyl 2-chloroacetoacetate (2a) and 2-bromoacetophenone (2b), respectively. The ORTEP drawings of compounds 8g, 8h and 9f provide strong evidence of the structure of aromatic thiazole derivatives 8a-h and 9a-h. Undoubtedly, the structure of compounds 3e-h and 4e-h synthesized by the reaction of 3-aryl-4-formylsydnone thiosemicarbazones 1e-h with cyclization reagents 2a and 2b in the previous work should have the thiazole moiety, and not the thiazoline moiety. Both the new thiazole derivatives 8a-h and 9a-h and the 3-arylsydnonyl-substituted derivatives 3e-h and 4e-h were investigated to determine their antioxidant activity by two tests that have been highly documented-the direct scavenging effect on a stable free 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and the inhibition of the 2,2-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) radical. Results of this study demonstrate that not only the thiazole ring and the aryl ring has the contribution to the antioxidant activities, the sydnone ring of 3-arylsydnonyl moiety also has its considerable contribution.     

Current perspectives on quinazolines with potent biological activities: A review

Quinazoline is a heterocyclic compound having biological activities. It is aromatic in nature having bicyclic structure containing benzene ring and pyrimidine ring. Quinazoline and its derivatives are found to have wide range of biological activities that is anticancer, analgesic, antimicrobial, antihypertensive, anticonvulsant, antimalarial, antitumor, and anti-tubercular activities. The purpose of this review is to highlight the recent researches made by researchers on various biological activities of quinazoline derivatives on different targets.