Combinations of Cyclodextrins with Synthetic and Natural Compounds

Host–guest compounds formed by cyclodextrins with synthetic and natural compounds are reviewed with regard to their properties, characterisation (using experimental and computational methods) and applications.     

双酰胺类化合物的合成及生物活性研究

为了寻找高活性农药先导化合物,以甲霜灵为先导,通过活性基团拼接原理,设计合成了一系列未见文献报道的双酰胺类化合物,其结构经1H NMR、13C NMR和HRMS表征.初步的生物活性测试结果表明:在50 mg/L测试浓度下,化合物5j对黄瓜霜霉病显示出85%的抑制率;在500 mg/L剂量下,多数目标化合物对粘虫表现出较好的杀虫活性,其中化合物5b,5f,5g,5h,5i,5l对粘虫的致死率高达100%,在250 mg/L测试浓度下,化合物5f,5h,51对粘虫的致死率为50%.     

苯并三氮唑类化合物的合成及生物活性

设计并合成了6种新的苯并三氮唑类化合物,其结构均经^1H NMR和IR确认。初步测定了其生物活性．结果表明6种化合物对小白菜的胚根、根和苗的生长均具有一定的调节作用。     

酰基脲类化合物的生物活性及合成方法

对酰基脲类化合物的生物活性及作用机理和常见的合成方法进行了介绍。酰基脲类化合物具有杀虫杀螨活性、植物生长调节活性和降低血糖等功能。其合成方法主要有异氰酸酯法和取代脲法等方法。     

The Anti-Leukemic Activity of Natural Compounds

The use of biologically active compounds has become a realistic option for the treatment of malignant tumors due to their cost-effectiveness and safety. In this review, we aimed to highlight the main natural biocompounds that target leukemic cells, assessed by in vitro and in vivo experiments or clinical studies, in order to explore their therapeutic potential in the treatment of leukemia: acute myeloid leukemia (AML), chronic myeloid leukemia (CML), acute lymphocytic leukemia (ALL), and chronic lymphocytic leukemia (CLL). It provides a basis for researchers and hematologists in improving basic and clinical research on the development of new alternative therapies in the fight against leukemia, a harmful hematological cancer and the leading cause of death among patients.     

离子型有机锡化合物的合成及其生物活性

利用有机锡卤化物与有机酸在有机胺存在下反应合成了一系列离子型有机锡化合物,分子通式为[HNR3][(PhCH2)3Sn(μ2-SCH2COO)Cl]、[HNR3][Ph3Sn)3(O2CCH2CO2)2]·CH3CH2OH和[HNR3] [MeCy2ClSnO2CCH2CO2SnClCy2Me]。化合物的体外抗肿瘤、杀菌和杀螨活性测试结果表明,部分化合物具有很好的生物活性。[HNR3][(Ph3Sn)3(O2CCH2CO2)2]·CH3CH2OH和[HNR3] [MeCy2ClSnO2CCH2CO2SnClCy2Me]配合物对人肺癌细胞株A-549、结肠癌细胞株HCT-8和肝癌细胞株Bel-7402的抑制率约为90%,[HNR3][MeCy2ClSnO2CCH2CO2SnClCy2Me]配合物对小麦赤霉、番茄早疫、芦笋茎枯、苹果轮纹、花生褐斑的杀死率都为100%,配合物[HNR3] [MeCy2ClSnO2CCH2CO2SnClCy2Me]的杀螨活性致死率大于90%。     

含氟吡啶羧酸酯类化合物的合成及生物活性

为了寻找具有生物活性的新化合物,以氟乙酸甲酯、氰乙酰胺和甲酸乙酯为起始原料,经环合、氯化、水解、酰氯化等反应合成了含氟吡啶酰氯中间体,再与醇类和酚类反应合成了一系列含氟吡啶羧酸酯类化合物,总收率约38%。其结构经1HNMR、13CNMR、IR、MS及元素分析测试技术确证。初步杀虫抑菌活性测试表明,部分化合物1e、1i、1j和1k在500mg/L浓度下,对淡色库蚊的杀死率在61.9%～100%之间,但对几种受试植物病菌的抑制活性很差。化合物1k活性最好,在500mg/L时对粘虫(armyworm)和淡色库蚊(culex mosquito)的杀死率均为100%。初步构效关系分析表明,芳杂环酚的该类化合物有较好的活性,而脂肪醇的该类化合物无活性。     

笼状双环磷酸酯类化合物的合成与生物活性研究

近年来,科学家们相继合成出高度对称结构的双环磷酸酯笼状化合物,并研究了它们的生物活性,这类化合物具有良好的杀虫抗菌活性,且有独特的活性机理,在医药、农药、纤维、树脂及石油工业中已得到了广泛应用,本文采用季戊四醇和苯乙腈为起始原料,以下列反应步骤设计合成了8个新型笼状双环磷酸酯衍生物I,[1′-硫(氧)代-2′,6′,7′-三三氧杂-1′-磷杂双环(2,2,2)辛烷基-4′-甲基]-4-烷基-4-苯基-4-氰基丁酸酯:     

新型二氮杂双环化合物的合成、表征及生物活性研究

以酮和硝基甲烷为原料,经3步反应合成了2种氮取代的二氮杂双环结构化合物N-二氯乙酰基-9-氧代-1,5-二氮杂二环[4.3.0]壬烷,采用红外光谱、核磁共振和元素分析对产物结构进行了表征。并利用土培法对化合物进行了初步的生物活性试验。结果表明,化合物能够减轻普施特对玉米的伤害。     

嘧啶基硫代脲酸酯类化合物的合成及生物活性

嘧啶类、硫脲类化合物大多具有广谱、高效的杀菌活性。为了寻找更为优秀的杀菌剂新品种,选用含氮杂环取代嘧啶与烷氧羰基异硫氰酸酯反应,合成了14个取代嘧啶基硫代脲酸酯,其中12个化合物为首次报道的新化合物。结构组成经元素分析、IR及1HNMR确认,并测定了它们对5种植物病菌的室内毒力作用,结果表明大部分化合物具有良好的抑菌和杀菌活性。这些参数对合成和筛选新的活性化合物提供了依据。     

芳基噻唑联哌啶酰胺类化合物的合成及生物活性

为了寻找具有生物活性的新型芳香基噻唑联哌啶酰胺类先导化合物,设计并合成了15个未见文献报道的芳基噻唑联哌啶酰胺类化合物,其结构经1HNMR、13CNMR和HRMS确证,生物活性测定结果显示,部分目标化合物表现出高效的抑菌和杀虫活性,如在200μg/mL浓度下,5-(3-溴苯基)-4-甲基-2-(1-((4-硝基苯基)磺酰基)哌啶-4-基)噻唑(6b)对黄瓜霜霉病的抑菌活性为100%,优于嘧菌酯,5-(4-溴苯基)-2-(1-((4-氯苯基)磺酰基)哌啶-4-基)-4-甲基噻唑(6c)对水稻纹枯病的抑菌活性为58.86%,与嘧菌酯相当;在500μg/m L浓度下,(4-(5-(3-溴苯基)-4-甲基噻唑-2-基)哌啶-1-基)(间甲基苯基)酮(6h)对粘虫的杀虫活性为100%.     

斯德酮类化合物的合成及生物活性研究

斯德酮类化合物的合成及生物活性研究李正名，范传文，王素华（南开大学元素有机化学研究所，元素有机化学国家重点实验室，天津，３０００７１）关键词斯德酮，合成，生物活性斯德酮（Ｓｙｄｎｏｎｅ）化合物是一类介－离子（Ｍｅｓｏ－ｉｏｎｉｃ）化合物，由于其结构有...     

Statistical Investigation into the Structural Complementarity of Natural Products and Synthetic Compounds

The potential of new natural products as an important source for the exploration and development of new drugs and crop protection products is a long way from being exhausted. The statistical analysis of the structures of the natural and synthetically derived compounds has shown conspicuous variations in structural types in the natural products derived from different natural sources, which can be utilized in the search for individual active substances. The occasionally voiced prepossession that natural products have already been sufficiently examined and therefore no more innovations are to be expected can definitely be rejected.     

Synthetic dsDNA‐Binding Peptides Using Natural Compounds as Model

We have developed a series of short DNA‐binding peptides containing newly synthesized, unnatural as well as natural amino acid building blocks. By a combinatorial‐library approach, oligopeptides were developed with moderate dsDNA‐binding affinities. Two strategies were used to further enhance the binding affinity of the lead peptides: Ac‐Arg‐Ual‐Sar‐Chi‐Chi‐Chi‐Arg‐NH₂ and Ac‐Arg‐Cbg‐Cha‐Chi‐Chi‐Tal‐Arg‐NH₂. Site‐selective amino acid substitutions increased the binding affinities up to 2 × 10^?5 M . Further enhancement of the binding affinities could be achieved by coupling of an acridine intercalating unit, using linker arms of different length and flexibility. With the introduction of a new lysine‐based acridine unit, different types of oligopeptide–acridine conjugates were designed using known dsDNA‐binding ligands as model compounds. The binding capacities of these new oligopeptide–acridine conjugates have been investigated by a fluorescent intercalator (ethidium bromide) displacement (FID) assay. With the synthesis of the dipeptide–acridine conjugates, binding affinities in the low micromolar range were obtained (6.4 × 10^?6 M ), which is similar to the binding strength of the well‐known DNA binder Hoechst 33258.     

苯基取代的苯并噻唑胺双苯甲酰胺衍生物的合成及生物活性

以取代苯甲酸和取代邻氨基苯甲酸为起始原料,设计合成了13个含取代苯并噻唑胺邻甲酰氨基苯甲酰胺类化合物,其结构经1H NMR、13C NMR、IR及元素分析确证。 初步生物活性测试结果表明,在500 mg/L目标化合物浓度下,对黄瓜花叶病毒有一定抑制作用。 采用MTT法进行化合物抑制PC3癌细胞体外活性测试,结果表明,所合成的化合物具有不同程度的抑制PC3癌细胞活性,其中化合物4f在10 μmol/L浓度下对PC3的抑制率为74.2%。     

吡唑腙及其双杂环化合物的设计、合成及生物活性

利用Vilsmeier-Haak反应得到活性中间体,取代-4-甲酰基吡唑;将其与芳氧乙酰肼反应,合成5个吡唑腙类化合物3,再经关环反应,制得5个吡唑类双杂环化合物4。所有新化合物的结构均经IR,1H NMR,MS和元素分析确证了结构。对新化合物3,4分别进行了棉花枯萎病菌、棉花黄萎病菌、棉花立枯病菌、瓜果腐霉病菌、番茄早疫病菌、向日葵菌核病菌等初步的抑菌活性测试,结果表明,吡唑类双杂环化合物4的抑菌效果明显高于吡唑腙化合物3。在质量浓度为50mg/L时,3d、3e对番茄早疫病菌、向日葵菌核病菌有较好的抑制效果(﹥80%);双杂环化合物4对6种病菌均有明显的抑制效果(﹥70%),其中4d、4e对棉花立枯病菌的抑制率大于95%。     

Antimicrobial and Antimalarial Activity of Novel Synthetic Mononuclear Ruthenium(II) Compounds

The present work was aimed that the two Ruthenium compounds namely, [Ru(A)₂(B)]Cl₂, where A = 1,10‐phenanthroline; B = 2‐NO₂‐phenyl thiosemicarbazone (Compound R₁)/2‐OH‐phenyl thiosemicarbazone (Compound R₂) have been tested for antibacterial activity at the concentrations of 1 mg/mL against various Gram‐Positive organisms (Lactobacillus, Staphylococcus pyrogenes, Bacillus subtilis, Staphylococcus aureus & Bacillus megatarium) and Gram‐Negative organisms (Pseudomonas aeruginosa, Escherichia coli, Proteus vulgaris, Enterobacter aerogenes, Salmonella paratyphi, Klebsiella pneumonia & Proteus mirabilis). The compounds were also tested for antifungal activity against Aspergillus clavatus, Aspergillus niger, Colletotrichum & Penicillium notatum by using agar diffusion assay and antimalarial activity against Plasmodium falciparum (Strain 3D7) using MTT assay. The results concluded that the compound R₁ exhibited significant antibacterial activity than R₂ against Gram‐Negative bacteria with zones of inhibition ranging from 15‐20 mm. and mild antibacterial activity against Gram‐Positive bacteria in comparison to tetracycline, streptomycin and rifampicin. These complexes were found to have moderate antifungal activity with no activity was however observed against Aspergillus niger. The compound, R₁ exhibited antimalarial activity at 10 μg/mL, whereas R₂ did not show antimalarial activity upto 50 μg/mL. Sensitivity to the compounds was greatest in the gram‐negative bacteria, followed by the gram‐positive bacteria and fungi.     

An Overview on Synthetic 2-Aminothiazole-Based Compounds Associated with Four Biological Activities

Amongst sulfur- and nitrogen-containing heterocyclic compounds, the 2-aminothiazole scaffold is one of the characteristic structures in drug development as this essential revelation has several biological activities abiding it to act as an anticancer, antioxidant, antimicrobial and anti-inflammatory agent, among other things. Additionally, various 2-aminothiazole-based derivatives as medical drugs have been broadly used to remedy different kinds of diseases with high therapeutic influence, which has led to their wide innovations. Owing to their wide scale of biological activities, their structural variations have produced attention amongst medicinal chemists. The present review highlights the recently synthesized 2-aminothiazole-containing compounds in the last thirteen years (2008–2020). The originality of this proposal is based on the synthetic strategies developed to access the novel 2-aminothiazole derivatives (N-substituted, 3-substituted, 4-substituted, multi-substituted, aryl/alkyl substituents or acyl/other substituents). The literature reports many synthetic pathways of these 2-aminothiazoles associated with four different biological activities (anticancer, antioxidant, antimicrobial and anti-inflammatory activities). It is wished that this review will be accommodating for new views in the expedition for rationalistic designs of 2-aminothiazole-based medical synthetic pathways.     

具有生理活性的天然螺缩酮化合物研究进展

螺缩酮类化合物广泛存在于自然界中, 它们表现出的很好的生理活性已引起各国科学家的兴趣. 对近年来天然存在的螺缩酮化合物的研究进展进行了总结, 描述了这类化合物的结构特征, 展望了在医药、农药等方面的潜在发展前景.