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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. 相似文献
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Sanjit Kanjilal Kaki Shiva Shanker Kotte Sagar Rao Kunduru Konda Reddy Bhamidipati V. S. K. Rao Kota B. Shiva Kumar Mannepalli L. Kantam Rachapudi B. N. Prasad 《European Journal of Lipid Science and Technology》2008,110(12):1175-1182
An efficient chemo‐enzymatic synthesis of ferulic acid‐based structured lipids mimicking triacylglycerol with a pendant phenolic moiety was carried out for the first time. Initially, ferulic acid was reduced to coniferyl alcohol, followed by its esterification with fatty acids. The key step in the synthesis was dihydroxylation of the olefinic side chain of coniferyl ester, which was eventually esterified with fatty acids to generate phenolic structured lipids. Two such compounds of varying fatty acid chain lengths were synthesized in good yield. Structural confirmation of both compounds is based on IR, 1H and 13C NMR, and MS techniques. The synthesized compounds were tested for in vitro antioxidant and antimicrobial activities. Both compounds exhibited moderate to good antioxidant activity. The phenolic structured lipid with only shorter‐chain fatty acids showed antibacterial activity. Both compounds did not show any antifungal activity. 相似文献
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噻吩类化合物主要分为α-衍生物和β-衍生物,其应用领域广泛,其中噻吩类化合物在农药方面就有很广泛的应用,主要用于杀菌和杀虫,外国的很多研究显示噻吩类化合物对蚊蝇类卵、鳞翅目昆虫、幼虫具有显著的光活化毒杀效应,鳞翅目幼虫的生长发育起到抑制作用。概述了被文献报道的具有杀虫活性的部分噻吩类化合物,并对其发展前景进行展望。 相似文献
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硒是人体必需的微量元素,在近几十年中,它已成为化学、生物学、医药学和环境科学等研究的热点。在农药方面对含硒化合物的研究较少。介绍了采用生物电子等排和活性基团拼合原理等合成的硒化合物及其农药活性,指出含硒化合物可能是农药开发的一个潜在的方向。 相似文献
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The exploration of structure–activity relationships (SARs) in chemical lead optimization is mostly focused on activity against single targets. Because many active compounds have the potential to act against multiple targets, achieving a sufficient degree of target selectivity often becomes a major issue during optimization. Herein we report a data analysis approach to explore compound selectivity in a systematic and quantitative manner. Sets of compounds that are active against multiple targets provide a basis for exploring structure–selectivity relationships (SSRs). Compound similarity and selectivity data are analyzed with the aid of network‐like similarity graphs (NSGs), which organize molecular networks on the basis of similarity relationships and SAR index (SARI) values. For this purpose, the SARI framework has been adapted to quantify SSRs. Using sets of compounds with differential activity against four cathepsin thiol proteases, we show that SSRs can be quantitatively described and categorized. Furthermore, local SSR environments are identified, the analysis of which provides insight into compound selectivity determinants at the molecular level. These environments often contain “selectivity cliffs” formed by pairs or groups of similar compounds with significantly different selectivity. Moreover, key compounds are identified that determine characteristic features of single‐target SARs and dual‐target SSRs. The comparison of compounds involved in the formation of selectivity cliffs often reveals chemical modifications that render compounds target selective. 相似文献
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咪唑和三唑醚类化合物的合成及生物活性 总被引:1,自引:0,他引:1
以2,4-二氯-α-氯代苯乙酮、取代甲苯、咪唑、三唑为起始原料,合成了9个咪唑醚类和16个三唑醚类化合物,所有化合物结构经1HNMR、IR和元素分析进行了确证,对化合物对马铃薯晚疫病菌(Phytophthoro infestans)和秧苗枯萎病菌(Phizoctonia)的抑菌活性进行了测定,测定表明,25个化合物都有不同程度的抑菌活性,其中Ⅲa、Ⅲb、Ⅲd、Ⅳg、Ⅴb、Ⅴc等6个化合物质量浓度为50 mg/L和10 mg/L时,对两种病菌的抑菌率达80%和50%以上,初步分析了化合物抑菌活性与结构的关系。 相似文献
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Dr. Ivan Bassanini Dr. Silvia Parapini Prof. Nicoletta Basilico Prof. Anna Sparatore 《ChemMedChem》2019,14(22):1940-1949
SAR studies on a set of novel hydrophilic C-2 aminopyridinyl riminophenazines bearing variously functionalized basic side chains at C-3 were conducted. The novel compounds were evaluated for in vitro activity against two different species of Leishmania promastigotes, intramacrophage Leishmania amastigotes, chloroquine-sensitive and chloroquine-resistant strains of P. falciparum, and also against mature-stage P. falciparum gametocytes. Their cytotoxicity was evaluated as well on BMDM cell lines. Most of the new compounds potently inhibited the growth of both genera of protozoa with IC50 values in the high nanomolar range and good selectivities versus mammalian cells. Besides their potent activity against asexual intraerythrocytic stages of P. falciparum, three compounds showed potential as transmission-blocking agents. The key role of the hydrophilic C-2 aminopyridinyl substituent to improve the leishmanicidal activity and the influence of the length and the nature of the basic side chain on the antiprotozoal activity and cytotoxicity were underlined. 相似文献
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Songul Kesen Hasim Kelebek Serkan Selli 《Journal of the American Oil Chemists' Society》2013,90(11):1685-1696
Volatile and phenolic compositions of olive oil obtained from the cv. Halhali were investigated in the present study. Fruits were harvested at the optimum maturity stage of ripeness and immediately processed with cold press. Simultaneous distillation/extraction (SDE) with dichloromethane was applied to the analysis of volatile compounds of olive oil. Sensory analysis showed that the aromatic extract obtained by SDE was representative of olive oil odour. In the olive oil, 40 and 44 volatile components were identified and quantified in 2010 and 2012 year, respectively. The total amount of volatile compounds was 18,007 and 19,178 μg kg?1 for 2010 and 2012, respectively. Of these, 11 compounds in the 2010 and 12 in the 2012 harvest presented odour activity values (OAVs) greater than 1, with 1‐octen‐3‐ol, ethyl‐3‐methyl butanoate, (E)‐2‐heptenal and (E,Z)‐2,4‐decadienal being those with the highest OAVs in olive oil. The high‐performance liquid chromatographic method coupled with diode‐array detection was used to identify and quantify phenolic compounds of the olive oil. A total of 14 phenolic compounds in both years were identified and quantified in olive oil. The major phenolic compounds that were identified in both years were hydroxytyrosol, tyrosol, elenolic acid, luteolin, and apigenin. Antioxidant activity of olive oil was measured using the DPPH and ABTS methods. 相似文献
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Surface Active Properties and Biological Activities of Novel Anionic Surfactant Based on Oxapyridazinone Derivatives
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Manal Mohamed El-Shahawi Alyaa Abou Sheashaa Shalaby Adel Mohy El-Din Gabre Abd El-Hamed Mahmoud Ghonim 《Journal of surfactants and detergents》2016,19(1):137-144
A series of novel oxapyridazinone derivatives has been synthesized via cyclization of the corresponding sodium salt of α‐sulfonated fatty acid hydrazide with chloroacetic acid in the presence of sodium acetate and acetic anhydride. The structures of the prepared compounds were elucidated using different spectroscopic and elemental analysis. The surface properties (surface tension, CMC value and area per molecule), the thermodynamic stability and antimicrobial activities of the prepared compounds were determined and compared to standard trade material Texapone® N‐70. The prepared compounds exhibit surface activity comparable to the standard and thus can be used as anionic surfactants. 相似文献
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[目的]对小果博落回中分离的普罗托品、隐品碱和别隐品碱中的十元氮杂环和苯环进行结构修饰,合成了17种普罗托品类生物碱,在确认其结构的基础上考查其体外杀虫活性。[方法]首先,采用ESI-MS、1H NMR和13C NMR等波谱技术对目标化合物的结构进行表征;接着,以伊维菌素为阳性对照,采用浸虫法分别测定了目标化合物在0.5、1 g/L时对兔痒螨和小麦红蜘蛛的体外杀灭活性。[结果]大多数化合物对兔痒螨和小麦红蜘蛛均显示了一定程度的杀灭活性。其中,待测物1的活性最佳,其对兔痒螨的致死率达71.7%;对小麦红蜘蛛的致死率为60.0%,校正致死率达57.1%。[结论]对目标化合物的结构及其杀虫活性进行分析,发现向十元氮杂环引入C=C键可显著提高该类化合物的杀螨活性;向13位引入羰基可提高它们杀灭小麦红蜘蛛的活性。为普罗托品类杀虫剂的研发提供了一定的理论依据。 相似文献
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Dr. Peter E. Cockram Callum A. Turner Prof. Alexandra M. Z. Slawin Prof. Terry K. Smith 《ChemMedChem》2022,17(4):e202100664
There is an urgent need for the development of new treatments against trypanosomatid parasites; the causative agents of some of the most debilitating diseases in the developing world. This work targets an interesting 6-5-6-6 fused carboline scaffold, accessing a range of substituted derivatives through stereospecific intramolecular Pictet–Spengler condensation. Modification of the cyclisation conditions allowed retention of the carbamate protecting group and gave insight into the reaction mechanism. Compounds’ bioactivities were measured against T. brucei, T. cruzi, L. major and HeLa cells. We have identified promising pan-trypanocidal lead compounds based on the core scaffold, and highlight key SAR trends which will be useful for the future development of these compounds as potent trypanocidal agents. 相似文献
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Dr. Bill C. Hawkins Dr. Lisa M. Lindqvist Duong Nhu Dr. Phillip P. Sharp Dr. David Segal Dr. Andrew K. Powell Dr. Michael Campbell Dr. Eileen Ryan Dr. Jennifer M. Chambers Dr. Jonathan M. White Dr. Mark A. Rizzacasa Dr. Guillaume Lessene Prof. David C. S. Huang Dr. Christopher J. Burns 《ChemMedChem》2014,9(7):1556-1566
The complex natural products silvestrol ( 1 ) and episilvestrol ( 2 ) are inhibitors of translation initiation through binding to the DEAD‐box helicase eukaryotic initiation factor 4A (eIF4A). Both compounds are potently cytotoxic to cancer cells in vitro, and 1 has demonstrated efficacy in vivo in several xenograft cancer models. Here we show that 2 has limited plasma membrane permeability and is metabolized in liver microsomes in a manner consistent with that reported for 1 . In addition, we have prepared a series of analogues of these compounds where the complex pseudo‐sugar at C6 has been replaced with chemically simpler moieties to improve drug‐likeness. Selected compounds from this work possess excellent activity in biochemical and cellular translation assays with potent activity against leukemia cell lines. 相似文献
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