萜烯肟醚衍生物的合成及生物活性研究

探讨了萜烯肟醚的合成方法,合成了8个新型萜烯肟醚类化合物,并经元素和核磁确证结构.初步生物活性测试显示：部分化合物具有较好的杀菌活性.     

肟醚(酯)农药活性化合物的研究与开发进展

概述了具有虫、菌、草等广谱生物活性的肟醚(酯)化合物，重点介绍了具有肟醚(酯)结构农药的研究与开发进展以及其结构特点和活性特点，并对肟醚(酯)化合物的几何异构与其生物活性的关系及几何异构体的相互转化进行了简述。     

1，1＇-二芳基烷基醚化合物的合成及生物活性

在农药中，醚类结构常常被选为有效的活性基团。如以苯草醚、嘧草醚等为代表的二芳基醚类除草剂，以多来宝、溴氟醚菊酯等为代表的1，2’-二芳基烷基醚类杀虫剂等。但1，1’-二芳基烷基醚化合物作为农药的应用尚未见报道。笔者在从事具有杀虫活性的芳基烷基肟醚化合物的研究过程中，得到较高分子量的副产物，经结构及生物活性研究，     

肟醚类拟除虫菊酯立体有择合成

某些烷基芳基酮肟苯氧基苄醚化合物具有拟除虫菊酯杀虫特性。我们曾合成以下结构肟醚类化合物,研究其合成方法、结构特性及生物活性。     

含吡啶环肟醚化合物的合成及生物活性

研究了含吡啶环的肟醚化合物的合成及所合成化合物的生物活性     

氯苯肟唑(SPRI-WM-005)异构体的分离及其杀菌活性

氯苯肟唑（SPRI-WM-005）是含顺、反异构体的肟醚结构化合物。为了研究两个异构体及未分离的混合物在生物活性上是否存在差异，对两个异构体进行了分离，并做了对黄瓜白粉病的室内生物活性测定。结果表明，当处理剂量为50mg／L时，氯苯肟唑（Z，E混合物）、Z-氯苯肟唑和E-氯苯肟唑的防效分别为95％、100％和97％，三者活性基本相当，故在实际中无须将两个异构体分离，混合体可直接应用。     

含二茂铁基肟醚类化合物的合成及抗真菌活性

以二茂铁为起始原料,合成了3-二茂铁基-5-芳基吡唑啉,再依次与氯乙酰氯和醛肟反应,生成16个二茂铁基肟醚类化合物。通过~1HNMR、FT-IR及ESI-HRMS对目标化合物进行结构表征。将合成的肟醚类化合物分别对3种植物真菌病(马铃薯干腐病、烟草赤星病、西瓜枯萎病)进行了初步的抗植物真菌活性实验。测试结果显示,部分化合物具有良好的抗植物真菌活性。     

杂环羰基肟类化合物的合成及杀虫活性研究

以取代苯胺为原料合成对位全氟烷基取代的苯胺,以乙酰基杂环为原料合成关键中间体杂环芳基-α-氯代-α-羰基肟(VI),在原有肟醚类化合物结构基础上引入全氟烷基设计合成了12个未见报导的含全氟烷基的杂环羰基肟类化合物,并通过~1H NMR和MS对所有目标化合物进行了结构确认,进行生物活性测试。初步结果表明:部分化合物对苜蓿蚜表现出一定的活性,化合物ZJ2、ZJ3和ZJ8在500 mg/L浓度下对苜蓿蚜的致死率达到90%。     

新型具有含硫肟醚基的苯甲酰脲类化合物的合成及其杀虫活性研究

通过含硫不饱和肟醚与2，6-二氟苯甲酰异酯反应，合成了9个新的具有含硫肟醚基的苯甲酰脲类化合物，其结构均经^1HNMR、IR、LC／MS及元素分析确证，检测结果表明部分化合物表现出很高的杀虫活性。     

具有杀虫活性的嘧啶类化合物的研究进展

在农药和医药领域,嘧啶类化合物是一类重要的活性物质。按照化合物结构的特点将具有杀虫活性的嘧啶类化合物归纳为嘧啶胺类、嘧啶(硫)醚类、稠环类和其他类嘧啶化合物,介绍了这几类化合物中具有较好杀虫活性的物质并对部分化合物的生物活性及创制经纬作了简要的概述。     

新型二氯丙烯类杀虫剂的合成及杀虫活性

在研究以往二氯丙烯类杀虫剂的基础上，保留化合物的活性部分，改变其它可变基团，研究开发出九种新结构的化合物，结构经^1HNMR确认。杀虫活性测试结果表明，新化合物与先导化合物S-1812相比，具有相同或更高的杀虫效果，而且部分化合物的杀虫谱更宽，活性更高。     

Synthesis and Evaluation of Bis‐Thiazolium Salts as Potential Antimalarial Drugs

An innovative therapeutic approach based on the use of dicationic derivatives was previously designed to inhibit the biosynthesis of phosphatidylcholine in Plasmodium spp. Among these, bis‐thiazolium salts were shown to block proliferation of the malaria parasite at concentrations in the low nanomolar range. However, due to unsuitable molecular properties such as the presence of the two polar heads and flexibility in the linker, these compounds have low oral bioavailability. To characterize the structural requirements of the linker that lead to more rigid analogues with fewer rotatable bonds but which retain antimalarial activity, a new series of compounds incorporating an aryl moiety and eventually oxygen atoms were prepared, and their biological activity was evaluated. Structure–activity relationships suggest that the optimal linker construct is an aromatic group with two n‐butyl chains branched at the para position; two new leads (compounds 39 and 40 ) were selected for further development.     

Synthesis and Evaluation of a Series of Bis(pentylpyridinium) Compounds as Antifungal Agents

A series of bis(4‐pentylpyridinium) compounds with a variety of spacers between the pyridinium headgroups was synthesised, and the antifungal activity of these compounds was investigated. Lengthening the alkyl spacer between the pentylpyridinium headgroups from 12 to 16 methylene units resulted in increased antifungal activity against C. neoformans and C. albicans, but also resulted in increased hemolytic activity and cytotoxicity against mammalian cells. However, inclusion of an ortho‐substituted benzene ring in the centre of the alkyl spacer resulted in decreased cytotoxicity and hemolytic activity, while maintaining antifungal potency. Replacement of the alkyl and aromatic‐containing spacers by more hydrophilic ethylene glycol groups resulted in a loss of antifungal activity. Some of the compounds inhibited fungal PLB1 activity, but the low correlation of this inhibition with antifungal potency indicates PLB1 inhibition is unlikely to be the predominant mode of antifungal action of this class of compounds, with preliminary studies suggesting they may act via disruption of fungal mitochondrial function.     

Phytotoxicity of Vulpia Residues: III. Biological Activity of Identified Allelochemicals from Vulpia myuros

Twenty compounds identified in vulpia (Vulpia myuros) residues as allelochemicals were individually and collectively tested for biological activity. Each exhibited characteristic allelochemical behavior toward the test plant, i.e., inhibition at high concentrations and stimulation or no effect at low concentrations, but individual activities varied. Allelopathins present in large quantities, such as syringic, vanillic, and succinic acids, possessed low activity, while those present in small quantities, such as catechol and hydrocinnamic acid, possessed strong inhibitory activity. The concept of a phytotoxic strength index was developed for quantifying the biological properties of each individual allelopathin in a concise, comprehensive, and meaningful format. The individual contribution of each allelopathin, assessed by comparing the phytotoxic strength index to the overall toxicity of vulpia residues, was variable according to structure and was influenced by its relative proportion in the residue. The majority of compounds possessed low or medium biological activity and contributed most of the vulpia phytotoxicity, while compounds with high biological activity were in the minority and only present at low concentration. Artificial mixtures of these pure allelochemicals also produced phytotoxicity. There were additive/synergistic effects evident in the properties of these mixtures. One such mixture, formulated from allelochemicals found in the same proportions as occur in vulpia extract, produced stronger activity than another formulated from the same set of compounds but in equal proportions. These results suggest that the exploration of the relative composition of a cluster of allelopathins may be more important than simply focusing on the identification of one or two compounds with strong biological activity and that synergism is fundamental to the understanding of allelopathy.     

对有潜力作为生物农药物质的新研究

介绍了一些已知有非农药用途活性的生物发酵液和其活性物质的农药活性的最新研究，其中一些物质对病虫害的作用可与商业化制剂媲美。指出对已有各种用途天然源物质进行生物农药开发研究是开发农药的一个重要的途径。     

Antimicrobial Activity of 1,3,4-Oxadiazole Derivatives

The worldwide development of antimicrobial resistance forces scientists to search for new compounds to which microbes would be sensitive. Many new structures contain the 1,3,4-oxadiazole ring, which have shown various antimicrobial activity, e.g., antibacterial, antitubercular, antifungal, antiprotozoal and antiviral. In many publications, the activity of new compounds exceeds the activity of already known antibiotics and other antimicrobial agents, so their potential as new drugs is very promising. The review of active antimicrobial 1,3,4-oxadiazole derivatives is based on the literature from 2015 to 2021.     

2-芳醛腙噻唑类化合物的合成及其抗肿瘤活性

噻唑环和腙键结构均具有一定的生物活性,采用活性结构拼接法,将噻唑环与腙键相结合,设计并合成了16个2-芳醛腙噻唑类化合物,并采用MTT法对目标化合物进行体外抗肿瘤活性筛选。测试结果表明,该类新化合物对乳腺癌细胞株(MDA-MB-231、MDA-MB-468、MCF-7)具有一定的抗增殖活性。其中,N-(2-吡啶)甲醛-2-(4-苯基)噻唑腙的抗增殖活性最好,其IC50值分别为(0.21±0.11)、(0.18±0.10)、(0.17±0.08)μmol/L;而该化合物对其他肿瘤细胞亦具有一定的抗增殖活性,且相对乳腺癌细胞株的生物活性均在10倍及以上,说明其对乳腺癌细胞具有较好的生物活性和选择性,且毒副作用小,值得作为抗乳腺癌先导化合物进行进一步研究。     

新型杀虫剂取代-2-硝基亚氨基-咪唑烷的合成及初步药效试验

采用类同合成法对吡虫啉分子结构进行改造，合成出了5个新取代－2－硝基亚氨基－咪唑烷化合物，并且对这5个化合物用萝卜蚜进行了初步药效试验，发现5个化合物都有不同程度的药效，显示出其均可作为先导化合物，从而进一步优化分子结构开发成为一种高效、低毒、较低成本新农药的良好前景。     

Preparation, characterization, and surface and biological properties of N-stearoyl amino acids

Several lipoamino acids were synthesized, in which n-octadecanoic acid (stearic acid) was coupled with the α-amino group of an amino acid. The products were characterized and their identities confirmed by advanced analytical techniques like Fourier transform infrared ¹H nuclear magnentic resonance spectroscopy, and differential scanning, calorimetry. Their surface properties, such as critical micelle concentration (CMC) and foaming properties, biodegradability, and antimicrobial activity were also evaluated. The N-stearoyl amino acids (NSA) had low CMC values, and some of them showed good foaming properties. They were screened for antimicrobial activity against the gram-positive bacteria Staphylococcus aureus, Micrococcus luteus, and Bacillus cerceus, the gram-negative bacteria Escherichia coli and Pseudomonas aeruginosa, and the yeast Candida albicans. All the compounds inhibited at least one of these organisms. N-Stearoyl proline was the most effective, the order of antimicrobial activity being aromatic NSA> acidic NSA>basic NSA. However, the effective inhibition by all the compounds indicates the desirability of more thorough investigation and suggests that some of these compounds may have potential utility as biostatic additives in commercial products. All NSA are highly biodegradable and can readily be removed under conditions of normal secondary sewage treatment.     

吡唑席夫碱化合物的合成及其生物活性研究

以乙酰丙酮、水合肼、取代苯甲醛为起始原料,经过肟化、缩合反应得到一系列新型吡唑席夫碱化合物,通过元素分析、。HNMR、FTIR、MS等对目标化合物结构进行表征,并采用平皿法测试了目标化合物对单子叶植物玉米的生长调节活性。结果表明,目标化合物在低浓度下对玉米的生长表现出促进作用,尤以10mg·L-1浓度下对玉米生长的促进作用最显著,高浓度下对玉米的生长表现出显著抑制作用。