1,4-戊二烯-3-酮衍生物在农药创制中的应用进展

1,4-戊二烯-3-酮衍生物作为一种重要的天然姜黄素衍生物,具有抗病毒、抑菌、杀虫、抗氧化、抗癌、消炎等较为广泛的生物活性,在医药和农药的创制中发挥着重要作用。综述了近年来1,4-戊二烯-3-酮衍生物在农药创制方面的研究进展,主要包括通过醚化和肟化来创制具有抗病毒、抑菌、杀虫等生物活性的活性药性分子,以期望对研究工作者有一定的启发。     

哒嗪衍生物在农药活性方面的研究进展

哒嗪化合物因具有抑菌、杀虫、除草和抗病毒等生物活性而引起广泛关注,通过结构修饰将不同基团引入到哒嗪结构中,能产生具有广谱生物活性的化合物,使其在新型高效农药创制中起着重要的作用。按其在农药应用方面的不同活性作用进行分类,综述了哒嗪衍生物在抑菌、杀虫杀螨、除草及抗病毒方面的应用,并展望了该类化合物的发展趋势和应用前景。     

1,2,3-噻二唑类化合物农药生物活性的研究进展

1,2,3-噻二唑类化合物因具有抑菌、杀虫、除草和抗病毒等生物活性而引起广泛关注,通过结构修饰将不同基团引入到1,2,3-噻二唑结构中,能合成具有广谱生物活性的化合物,使其在新型高效农药创制中起着重要的作用。综述了1,2,3-噻二唑衍生物在农药活性方面的应用,并展望了该类化合物的发展趋势和应用前景。     

酰胺类化合物农药生物活性的研究进展

酰胺类化合物因具有抑菌、杀虫、除草和抗病毒等生物活性而引起广泛关注,通过结构修饰将不同基团引入到酰胺结构中,合成具有广谱生物活性的化合物,使其在新型高效农药创制中起着重要的作用。按其在农药生物活性方面进行分类,综述了酰胺衍生物在抑菌、杀虫杀螨、除草及抗病毒方面的应用,并展望了该类化合物的发展趋势和应用前景。     

1,3,4-噻二唑类衍生物的农药活性研究进展

1,3,4-噻二唑类化合物因具有杀菌、杀虫、除草和抗病毒等生物活性而引起广泛关注,通过结构修饰将不同基团引入到1,3,4-噻二唑结构中,得到具有广谱生物活性的化合物,使其在新型高效农药创制中起着重要的作用。按其农药生物活性进行分类,综述了1,3,4-噻二唑衍生物在抑菌、杀虫杀螨、除草及抗病毒方面的应用,并展望了该类化合物的发展趋势和应用前景。     

1,3,4-噁二唑衍生物在农药活性中的研究进展

1,3,4-噁二唑类化合物因具有抗抑菌、杀虫、除草和抗病毒等生物活性而引起广泛关注,通过结构修饰将不同基团引入到1,3,4-噁二唑结构中,能合成具有更广谱生物活性的化合物,使其在新型高效农药创制中起着重要的作用。按其拼接的结构进行分类,综述了1,3,4-噁二唑衍生物在抑菌、杀虫杀螨、除草及抗病毒方面的研究进展,并展望了该类化合物的发展趋势和应用前景。     

具有农药活性物1,3,4-噁二唑硫醚类化合物研究进展

1,3,4-噁二唑硫醚衍生物具有广谱生物活性,从抑菌、杀虫、除草及抗病毒等农药活性方面综述了1,3,4-噁二唑硫醚类化合物研究进展,期望为1,3,4-噁二唑硫醚衍生物在农业方面的应用提供依据。     

喹唑啉衍生物在农药活性方面的研究进展

喹唑啉化合物因具有广泛的生物活性,在农药领域受到越来越多的关注。通过结构修饰将不同药效基团引入到喹唑啉结构中,能产生一系列具有广谱生物活性的化合物,使其在新型高效农药创制中起着重要的作用。综述了喹唑啉衍生物在抑菌、杀虫杀螨、除草及抗病毒方面的研究进展,并展望了该类化合物的发展趋势和应用前景。     

二氢杨梅素衍生物的研究进展

二氢杨梅素属黄酮类物质,具有抗肿瘤、抗炎及护肝等作用,可用于食品药品等领域,但在应用中存在一定的局限性,如溶解性较差、抗氧化活性不佳、稳定性差等。对二氢杨梅素的酯化物、酰化物、金属配合物及糖苷化物进行总结,其衍生物的溶解性、抗氧化活性、稳定性及抑菌活性等有所改善。     

氰基丙烯酸酯类化合物的生物活性研究进展

氰基丙烯酸酯类化合物是一类高活性的PSⅡ电子传递抑制剂,由于它作用机制新颖、环境友好,故其分子设计、合成及生物活性成为目前农药创制的热点之一,按其在农药应用方面的不同活性作用进行分类,综述了近年来氰基丙烯酸酯衍生物的除草、杀菌和抗病毒活性的研究进展.     

喹啉及其衍生物的合成与生物活性研究进展

喹啉及其衍生物具有广泛的生物活性如抗HIV、抗癌、抗病毒及杀菌等,显示了广泛的应用前景。综述了近年来喹啉及其衍生物的合成方法及生物活性的研究进展。     

吡唑啉类化合物生物活性及研究进展

吡唑啉衍生物具有抗菌、抗炎、抗变形虫、抗肿瘤等生物活性,在医药与农药创制中占有重要地位。根据吡唑啉衍生物在医药与农药中的用途进行分类,对其生物活性进行介绍,并对其发展前景作进一步展望。     

生漆中漆酚单体分离、化学结构修饰及生物活性研究进展

漆酚化合物是具有C₁₅或C₁₇烃基侧链的邻苯二酚结构,侧链不饱和度为0~3。漆酚良好的抗肿瘤、抑菌和抗氧化活性使其受到越来越多的关注。对不同不饱和度烃基漆酚单体的分离方法进行了叙述,介绍了通过对漆酚的苯环或侧链烃基进行化学结构修饰这2种途径以获得结构相对稳定的漆酚衍生物,并阐述了漆酚单体及其衍生物的抗肿瘤、抗氧化、抑菌和抗病毒等生物活性。     

Updated Information on Antimicrobial Activity of Hydrazide–Hydrazones

Hydrazide–hydrazones possess a wide spectrum of bioactivity, including antibacterial, antitubercular, antifungal, anticancer, anti-inflammatory, anticonvulsant, antidepressant, antiviral, and antiprotozoal properties. This review is focused on the latest scientific reports regarding antibacterial, antimycobacterial, and antifungal activities of hydrazide–hydrazones published between 2017 and 2021. The molecules and their chemical structures presented in this article are the most active derivatives, with discussed activities having a hydrazide–hydrazone moiety as the main scaffold or as a side chain. Presented information constitute a concise summary, which may be used as a practical guide for further design of new molecules with antimicrobial activity.     

Recent Development of Pyrimidine-Containing Antimicrobial Agents

Multidrug-resistant bacterial infections have become an important cause of clinical death in the twenty-first century. Much effort has been made to overcome this challenge. The discovery of novel antimicrobial compounds, as well as the rational use of antibacterial drugs with different structure types and mechanisms, is helping to deal with bacterial resistance. Currently, pyrimidine-containing agents are the major areas of new antibacterial drug discovery. Given their good activities and diverse mechanisms of action, many pyrimidine-containing heterocyclic compounds have become the focus of interest for many scientists. In addition, pyrimidine structure is an important part of many endogenous substances, which is an advantage that allows pyrimidine derivatives to interact with genetic materials, enzymes and other biopolymeric substances in the cell. Scientists have focused on the discovery and structural optimization of pyrimidine derivatives, which has resulted in the discovery of many novel pyrimidine derivatives with intriguing profiles. Herein we summarize the therapeutic potentials of pyrimidine compounds that are promising for antimicrobial applications over the last decade. In particular, the relationships between the structures of modified pyrimidines and their antimicrobial activity are systematically discussed.     

Antioxidant activity of flavonol aglycones and their glycosides in methyl linoleate

The antioxidant activities of the flavonol aglycones, quercetin and myricetin, and their selected glycosides were compared in bulk methyl linoleate oxidized at 40°C. Methyl linoleate hydroperoxide formation, hydroperoxide isomer distribution, and ketodiene formation were followed by using high-performance liquid chromatography (HPLC) analysis. The aglycones, quercetin and myricetin, were consistently more active in bulk methyl linoleate than their glycosides and more active than α-tocopherol at 500 and 1000 μM. At 50 μM, the order of activity was myricetin > α-tocopherol > quercetin, and the order of activity of quercetin and its derivatives was quercetin > quercitrin > isoquercitrin > rutin. Myricitrin was slightly less active than myricetin. The sugar moiety was shown to have a marked effect on the antioxidant activity of flavonols. The rhamnoside derivatives, quercitrin and myricitrin, both possessed activity close to that of their corresponding aglycones. The different activities of glycosides could be partly explained by different solubilities and by differences in oxidizability of glycosides containing a monosaccharide or disaccharide at the C₃ position. The effect on hydroperoxide isomer distribution indicates that α-tocopherol was a more effective hydrogen donor than flavonoids, although flavonoids were more effective in inhibiting oxidation of methyl linoleate.     

Recent Development of Benzimidazole‐Containing Antibacterial Agents

Clinically significant antibiotic resistance is one of the greatest challenges of the twenty‐first century. However, new antibacterial agents are currently being developed at a much slower pace than our growing need for such drugs. Given their diverse biological activities and clinical applications, many bioactive heterocyclic compounds containing a benzimidazole nucleus have been the focus of interest for many researchers. The benzimidazole nucleus is a structural isostere of naturally occurring nucleotides. This advantage allows benzimidazoles to readily interact with the various biopolymers found in living systems. In view of this situation, much attention has been given to the exploration of benzimidazole‐based antibacterial agents, leading to the discovery of many new chemical entities with intriguing profiles. In this minireview we summarize novel benzimidazole derivatives active against various bacterial strains. In particular, we outline the relationship between the structures of variously modified benzimidazoles and their antibacterial activity.     

The development of FtsZ inhibitors as potential antibacterial agents

The emergence and prevalence of bacterial resistance has resulted in a clear demand for novel antibacterial drugs. As a tubulin homologue, FtsZ is an essential cell-division protein in prokaryotic organisms and is showing increasing promise as a target for antibacterial drug discovery. This review describes the role of FtsZ in bacterial cytokinesis and various FtsZ inhibitors, with particular focus on their discovery, antibacterial activities, mechanisms of action, synthetic methods, and representative analogues.     

Synthesis and Antibacterial Activities of 1-Alkyl-3-methacryloyl (Acryloyl) of Benzimidazolone (Thione) Derivatives

A series of (28) 1-alkyl-3-methacryloyl (acryloyl)-benzimidazolone (thione) deriv-atives were synthesized. The structures of the new derivatives were confirmed by (1)H-NMR, (13)C-NMR and ESI-MS spectral analysis. The antibacterial activities of these compounds against several strains of bacteria, such as Bacillus cereus, Bacillus subtilis, Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa, were evaluated by methods of paper disc-diffusion and broth mciro-dilution. Methacryloyl derivatives displayed higher antibacterial activities against tested bacterial strains than those of acryloyl derivatives in in vitro tests. A structure-activity relationship (SAR) study revealed that the presences of the methacryloyl moieties is essential to the antibacterial activities of the compounds.     

木脂素的生物合成及其微生物法生产的研究进展

木脂素是一类分布于植物中的次级代谢产物,由两分子苯丙素衍生物聚合而成。木脂素具有抗细菌、抗病毒和抗真菌活性,被广泛用于药物和食品中。目前,木脂素的生产主要依赖于植物提取。植物生长周期长、木脂素含量低等问题,限制了木脂素的商业应用。随着木脂素合成路径和关键酶的不断解析,木脂素的生物催化合成过程受到了越来越多的关注。本文总结了典型木脂素的生物活性、生物合成路径和微生物法生产的研究进展,可以为深入研究木脂素的微生物合成提供参考。