具有杀菌活性的5-三氟甲基取代■二唑类化合物研究进展

5-三氟甲基取代■二唑类化合物对大豆锈病具有良好的防效。根据结构特点可将该类化合物划分为S-1、S-2、S-3、S-4及其他类,并根据其结构类别的不同,对该类化合物的研究进展进行了概述。     

具有杀螨活性的三氟乙基硫醚(亚砜)类化合物研究进展

三氟乙基硫醚(亚砜)类化合物具有良好的杀螨活性。根据结构类别对其进行了综述,同时对该类化合物的研究趋势进行了展望,旨在为该类化合物的相关研究提供思路和依据。     

二萜类化合物微生物转化研究进展

二萜类化合物是一类重要的天然产物,研究发现微生物能对该类化合物进行多种类型的结构修饰。本文根据十年来二萜类化合物生物转化研究的报道,对二萜类化合物的生物转化菌种及催化反应类型进行综述,以期为二萜类化合物生物转化研究与应用提供参考。     

酰肼类昆虫生长调节剂的研究进展

综述了酰肼类昆虫生长调节剂的研究进展状况．讨论了该类化合物的结构与活性的关系。简单地介绍了该类化合物的作用机制,并依据文献总结出6条合成酰肼类化合物的方法,对该类化合物的发展前景做了展望。     

苯胺基喹唑啉类化合物的结构分析研究

喹唑啉类化合物是一类具有较好生物活性的化合物。对其结构进行了核磁、红外、紫外波谱研究,为更好地研究该类化合物的结构提供了参考。     

硫脲衍生物在农药活性方面的研究进展

硫脲类化合物因具有独特的生物活性在农药领域受到广泛关注。根据活性基团拼接原理,在硫脲基团上引入其他活性基团,通过结构修饰和优化期望生成一系列广谱活性的化合物,在新农药的创制中占据着重要的作用。综述了近几年具有良好抗病毒、杀虫、抗菌及除草活性的硫脲类化合物的研究进展,并对该类化合物的发展趋势和应用前景进行了展望。     

查尔酮类衍生物在农药活性方面的研究进展

查尔酮类化合物因具有杀菌、杀虫、除草和抗病毒等生物活性成为研发的热点,通过结构修饰将不同结构的药效团引入查尔酮结构中,设计了合成具有广谱生物活性的化合物,在新农药的研究与开发中发挥重要的作用。笔者对该类化合物在农药生物活性方面进行了分类,综述了查尔酮衍生物在抑菌、杀虫杀螨及抗病毒方面的研究成果,并展望了该类化合物的发展趋势和应用前景。     

C(2)位螺环氧化吲哚化合物合成研究进展

C(2)位螺环氧化吲哚化合物存在于许多天然生物碱和生物活性物质中,具有多种生物活性,由于结构新颖、独特且合成难度较大,因此该类化合物的合成引起了有机化学家和药物化学家的关注。在对近几年来氧化吲哚C(2)位螺环化合物合成方法调研的基础上,分别以过渡金属催化、高价碘试剂介导催化、有机催化、酸碱介导催化重排、光催化和其他催化等不同合成方法进行分类介绍该类化合物的研究进展,以期为该类化合物的后续研究提供参考。     

1,2,4-三唑类化合物的在医药活性方面的研究进展

1,2,4-三唑是含有2个氮原子的五元杂环,此类化合物具有抑菌、抗癌、抗肿瘤、抗炎等多种药理活性,通过结构修饰将不同基团引入到1,2,4-三唑结构中,能合成具有广谱生物活性的化合物,使其在医药领域具有广泛的应用。按其在医药生物活性方面进行分类,综述了近几年该类化合物的抑菌、消炎和抗癌活性的的研究进展,并对该类化合物的发展趋势和应用前景进行了展望。     

3-溴香豆素磺酰脲类化合物降血糖活性的定量构效关系研究

研究了3-溴香豆素磺酰脲类化合物降血糖活性与化学结构之间的关系,为进一步设计合成该类化合物提供理论依据。研究方法是首先选择14个化合物进行药效学研究,然后再对这些化合物利用MM2分子力学计算有关结构参数并进行定量构效关系研究,研究结果表明3-溴香豆素磺酰脲的降血糖活性与化合物的最小能量呈负相关,初步结论是该类化合物脲基取代基为脂肪基时,化合物的能量相对较小,降血糖活性较高。     

Untersuchungen zur Knüpfung der Peptidbindung mit α-trifluormethylsubstituierten α-Aminosäuren

Chemical Peptide Bond Formation with α-Trifluoromethyl Substituted α-Amino Acids The reaction of α-trifluoromethyl substituted N-^tbutoxycarbonyl amino acids (Boc-TFM-Xaa-OH) 1 with dicyclohexylcarbodiimide results in formation of 2-^tbutoxy-4-trifluoromethyl-5(4H)-oxazolones 2 within minutes. Compounds 2 react with amino acid esters to give Boc protected dipeptide esters 4. However, at room temperature compounds 2 decompose to give Leuchs anhydrides 3 , via retro ene reaction. Therefore, α-trifluoromethyl substituted N-^tbutoxycarbonyl amino acids (Boc-TFM-Xaa-OH) are of limited value for peptide synthesis.     

Synthese von N,N-pentamethylen-thiocarbamidsäure-S-(1-benzoyl-2,2-bis-methylthio)-vinylestern und deren Reaktionen mit N-Nucleophilen

Synthesis of S-(1-Benzoyl-2-bis-methylthio)-vinyl N,N-Pentamethylene-thiocarbamates and Their Reactions with N-Nucleophiles The S-(1-benzoyl-2-bis-methylthio)-vinyl-N,N-pentamethylene-thiocarbamates 3a – d are synthesized by reaction of S-phenacyl-N,N-pentamethylene-thiocarbamates ( 1a – d ) with carbon disulfide under phase-transfer conditions. These compounds 3a – d and the dithiocarbamates 5a – d react with N-nucleophiles forming the ketene-S,N-acetals 6 – 14 , the S-phenacyl α-(imidazolidine-2-ylidene)-N,N-pentamethylene-thio- or -dithiocarbamates 15 – 22 , S-(substituted pyrazol-4-yl)- 23 – 28 and S-(substituted isoxazol-4-yl)-N,N-pentamethylene-thio- or -dithiocarbamates 39 – 46 , respectively.     

Reaktionen mit Thio-bis-formamidinen

Reactions with Thio-bis-formamidines N,N,N′-Trisubstituted S-(4-amino-s-triazin-2-yl)-isothioureas 3 are prepared in good yields form trisubstituted thio-bis-formamidine-hydrochlorides 1 and esters of cyanimidocarboxylic acids 2 . In aqueous alkali solutions compounds 1 react with β-dicarbonyl compounds under rearrangement to yield substituted N-(pyrimidin-2-yl)-thioureas 4 and 5 .     

Untersuchungen zur proteasekatalysierten und chemischen Peptidbindungsknüpfung mit α-trifluormethylsubstituierten α-Aminosäuren

Protease Catalyzed and Chemical Peptide Bond Formation with α-Trifluoromethyl Substituted α-Amino Acids Subtilisin, α-chymotrypsin and papain catalyzed hydrolyses of α-trifluoromethyl substituted N-benzyloxycarbonyl amino acid methylesters (Z-TFM-Xaa-OMe) 1 can be achieved only in the case of 3,3,3-trifluoroalanine. Enzymatic incorporation of Z-TFM amino acids 2 into N-terminal position of dipeptides also fails. In contrary, dipeptides with a TFM amino acid moiety in N-terminal position, e.g. TFM-Phg-L-Phe-OMe 5 , react with H-Leu-NH₂ to give the corresponding tripeptides 6 in high yield. Z protected dipeptide derivatives 8 with N-terminal TFM amino acids can be obtained via 4-trifluoromethyl-5-(4H)-oxazolones 7 .     

Fatty Acids in Heterocyclic Synthesis. Part XIV: Synthesis of Surface Active Agents from Some Novel Class of Oxadiazole,Thiadiazole and Triazole Derivatives Having Microbiological Activities

Reaction of stearic acid with semicarbazide in refluxing POCl₃ afforded 2-amino-5-heptadecyl 1,3,4-oxadiazole. Acylation of the amino group with acetic anhydride, ethyl chloroacetate and chloroacetic acid gave amide and β-amino acid derivatives. These compounds were cyclized to imidazo[2,1-b]oxadiazole derivatives by two different techniques. Treating the starting oxadiazole compound with P₂S₅, hydroxyl amine and hydrazine hydrate in benzene afforded thiadiazole and triazole derivatives. Unexpectedly, triazolo[3,4-b][1,3,4]oxadiazole derivative was obtained when 1,3,4-oxadiazole derivative was refluxed with hydrazine hydrate in ethanol. The biological activities of the synthesized compounds were screened in vitro against some gram positive and gram negative bacteria and fungi. Addition of quantitative amount of propylene oxide units (3, 5, 7 mol) to the synthesized compounds afforded new nonionic surfactants. The physico-chemical and surface properties of the novel synthesized surfactants such as surface and interfacial tension, cloud point, wetting time, emulsion stability, foam height, CMC, resistance to hydrolysis and their biodegradability were investigated. In addition, surface parameters including effectiveness (π _CMC), efficiency (PC₂₀), maximum surface excess (Γ_max) and (A _min) were examined.     

3,5-二取代-1,2,4-(噁)二唑类衍生物的合成及生物活性

[目的]为了寻找具有良好生物活性的噁二唑类衍生物。[方法]以苯甲腈为原料,经加成、脱水环化等反应设计合成了一系列未见文献报道的噁二唑类衍生物,并对目标化合物进行了生物活性测试。[结果]其结构通过1H NMR、13C NMR和H RMS图谱得以确证。初步生物活性测试结果显示:部分目标化合物在质量浓度200 mg/L下对南方根结线虫有较好的抑制活性,其中化合物5f、6a、6b和6e对线虫的抑制率达到90%以上,尤其化合物4a、4d对线虫的抑制率达到100%,另外部分目标化合物对南方根结线虫和小菜蛾幼虫都具有一定的抑制活性。[结论]该类结构具有较好的生物活性,有进一步优化的潜力。     

Turn‐on chemosensors for silver ions based on oligomers with diaza‐16‐crown 6‐ether receptors and aromatic fluorophore end groups

The reaction of N‐(2,4‐dinitrophenyl)pyridinium chloride ( 1 ), diaza‐18‐crown 6‐ether (DA18C6) and 2,5‐bis(aminophenyl)‐1,3,4‐oxadiazole ( 2 ) caused the opening of the pyridinium ring and yielded an ionic oligomer (oligomer‐1) comprising a 5‐DA18C6‐penta‐2,4‐dienylideneammonium chloride main chain and 2‐(4‐aminophenyl)‐5‐phenyl‐1,3,4‐oxadiazole or 2‐(4‐N‐phenylpyridinium)‐5‐phenyl‐1,3,4‐oxadiazole end groups. Accordingly, the reaction of 1 , DA18C6 and 2,7‐diaminofluorene ( 3 ) yielded oligomer‐2. The structures of oligomer‐1 and oligomer‐2 were determined by comparing their ¹H NMR spectra with those of model compounds, which were synthesized by the 1:1 reaction of 1 with 2 or 3 . Oligomer‐1 and oligomer‐2 exhibited weak bluish‐green photoluminescence (PL) before the inclusion of Ag⁺ in the DA18C6 receptor, after which they exhibited strong bluish‐green PL. These observations can be explained by the occurrence of photoinduced electron transfer in the oligomers. Copyright © 2011 Society of Chemical Industry     

取代异噁唑甲酰基脲的合成及其抑菌活性

以5-甲基-3-(取代)苯基-4-异噁唑甲酰胺及取代苯胺为起始原料,经两步反应合成了10种N-取代苯基-5-甲基-3-(取代)苯基-4-异噁唑甲酰基脲新化合物,其结构经1HNMR、IR和元素分析确证。初步测试了目标化合物对番茄灰霉病菌和小麦纹枯病菌的室内抑菌活性,结果表明,部分化合物对番茄灰霉病菌表现出较好的抑菌活性。     

邻杂环(噁二唑)甲酰苯胺类化合物的设计合成及杀虫活性初步研究

以超高效杀虫剂氯虫苯甲酰胺为先导,在酰胺部分引入了邻杂环(噁二唑),设计并合成了16个含邻杂环(噁二唑)甲酰苯胺类新化合物。生测结果表明,化合物普遍具有高杀虫活性,在10 mg/L剂量下对小菜蛾的致死率均大于80%。本研究结果为该类化合物的创制提供了参考。