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Matthias Goebel Dr. Bart Staels Prof. Dr. Thomas Unger Prof. Dr. Ulrich Kintscher Prof. Dr. Ronald Gust Prof. Dr. 《ChemMedChem》2009,4(7):1136-1142
Probing SAR : The 1‐(biphenyl‐4‐ylmethyl)‐1H‐benzo[d]imidazole moiety is known to be an essential structural component of telmisartan for PPARγ activation. This study focused on the substituents at position 2 of the benzimidazole in an attempt to optimize PPARγ activation. In particular, the elongation of the alkyl chain and the introduction of an aromatic ring system were studied (shown).
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Radka Podlipn Martina Navrtilov Lucie Raisov Stuchlíkov Kateina Mokov Lenka Langhansov Lenka Sklov Barbora Szotkov 《International journal of molecular sciences》2021,22(13)
Although manure is an important source of minerals and organic compounds it represents a certain risk of spreading the veterinary drugs in the farmland and their permeation to human food. We tested the uptake of the anthelmintic drug fenbendazole (FBZ) by soybean, a common crop plant, from the soil and its biotransformation and accumulation in different soybean organs, including beans. Soybeans were cultivated in vitro or grown in a greenhouse in pots. FBZ was extensively metabolized in roots of in vitro seedlings, where sixteen metabolites were identified, and less in leaves, where only two metabolites were found. The soybeans in greenhouse absorbed FBZ by roots and translocated it to the leaves, pods, and beans. In roots, leaves, and pods two metabolites were identified. In beans, FBZ and one metabolite was found. FBZ exposure did not affect the plant fitness or yield, but reduced activities of some antioxidant enzymes and isoflavonoids content in the beans. In conclusion, manure or biosolids containing FBZ and its metabolites represent a significant risk of these pharmaceuticals entering food consumed by humans or animal feed. In addition, the presence of these drugs in plants can affect plant metabolism, including the production of isoflavonoids. 相似文献
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目的 建立QuEChERS结合超高效液相色谱-串联质谱法(ultra performance liquid chromatography -tandem mass spectrometry, UPLC-MS/MS)同时快速测定水产品中20种苯并咪唑类药物及其代谢物残留量的分析方法。方法 样品经乙腈提取, 用乙二胺-N-丙基甲硅烷(primary secondary amine, PSA)和中性氧化铝吸附剂净化, 通过Waters ACQUITY UPLC HSS T3 (2.1 mm×100 mm, 1.8 μm)色谱柱分离, 以0.1%甲酸水溶液-乙腈为流动相, 采用电喷雾正离子模式下, 多反应监测(multiple reaction monitoring, MRM)模式下分析, 基质匹配曲线外标法定量。结果 20种苯并咪唑类药物及其代谢物在0.05~20.00 μg/L范围内线性关系良好(r2≥0.9991), 在空白样品基质中进行3个不同浓度水平的加标实验, 平均回收率为63.3%~105.8%, 相对标准偏差为0.1%~7.5% (n=6)。方法检出限为0.1~0.5 μg/kg, 定量限为0.3~2.0 μg/kg。结论 该方法操作简便、灵敏度高、准确可靠, 适用于水产品中20种苯并咪唑类药物及其代谢物的快速筛查。 相似文献
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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. 相似文献
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Structure–Activity Relationships of 1,2‐Disubstituted Benzimidazoles: Selective Inhibition of Heme Oxygenase‐2 Activity 下载免费PDF全文
Dr. Xianqi Kong Dr. Dragic Vukomanovic Prof. Kanji Nakatsu Prof. Walter A. Szarek 《ChemMedChem》2015,10(8):1435-1441
Devising ways to up‐ or down‐regulate heme oxygenase activity is attracting much interest as a strategy for the treatment of a variety of disorders. With a view of obtaining compounds that exhibit high potency and selectivity as inhibitors of the heme oxygenase‐2 (HO‐2) isozyme (constitutive) relative to the heme oxygenase‐1 (HO‐1) isozyme (inducible), several 1,2‐disubstituted 1H‐benzimidazoles were designed and synthesized. Specifically, analogues were synthesized in which the C2 substituent was the following: (1H‐imidazol‐1‐yl)methyl, (N‐morpholinyl)methyl, cyclopentylmethyl, cyclohexylmethyl, or (norborn‐2‐yl)methyl. Compounds with the cyclic system in the C2 substituent being a carbocyclic ring, especially cyclohexyl or norborn‐2‐yl, and the N1 substituent being a ring‐substituted benzyl group, especially 4‐chlorobenzyl or 4‐bromobenzyl, best exhibited the target criteria of high potency and selectivity toward inhibition of HO‐2. The new candidates should be useful pharmacological tools and may have therapeutic applications. 相似文献
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Samia G. Ahmed Abd-El Hamid N. Ahmed Nabil M. Omar Mahmoud A. El-Gendy 《Journal of chemical technology and biotechnology (Oxford, Oxfordshire : 1986)》1993,57(4):363-370
The pyrimido[1,2-a]benzimidazole derivatives compounds 1–8 were synthesized through cyclocondensation of 2-aminobenzimidazole with the appropriate benzsubstituted benzoylacetone by fusion at 150–170°C for 5 h. Quaternary salts compounds 9–22 were obtained by quaternization of compounds 1–8 with dimethyl or diethyl sulfate and subsequent isolation as the relatively insoluble perchlorate salts. Assignment and confirmation of the structures of the newly synthesized compounds were based upon elemental microanalyses and other spectral evidence. 相似文献
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Gold Nanoparticle‐Based Paper Sensor for Simultaneous Detection of 11 Benzimidazoles by One Monoclonal Antibody 下载免费PDF全文
Lingling Guo Xiaoling Wu Liqiang Liu Hua Kuang Chuanlai Xu 《Small (Weinheim an der Bergstrasse, Germany)》2018,14(6)
A colloidal gold immunochromatographic assay based on a generic monoclonal antibody is developed for the simultaneous detection of benzimidazoles and metabolite residues in milk samples. The monoclonal antibody is prepared using 2‐(methoxycarbonylamino)‐3H‐benzimidazole‐5‐carboxylic acid as the hapten, and it can recognize 11 types of benzimidazoles simultaneously. The immunochromatographic strip is assembled and labeled using gold nanoparticles. This strip can detect 11 benzimidazoles including albendazole, albendazole s‐oxide, albendazole sulfone, fenbendazole, fenbendazole sulfone, flubendazole, mebendazole, parbendazole, oxfendazole, oxibendazole, and carbendazim within 15 min in milk samples. Results are obtained visually with the naked eye, and the cutoff values and the visual limit of detection values for these benzimidazoles are 25, 6.25, 12.5, 12.5, 50, 25, 50, 50, 50, 6.25, and 25 ng mL?1, and 6.25, 3.125, 3.125, 1.56, 12.5, 6.25, 12.5, 12.5, 6.25, 0.78, and 12.5 ng mL?1, respectively. Results are also obtained using a hand‐held strip scan reader, with calculated limit of detection values for these benzimidazoles of 0.83, 0.77, 1.83, 0.98, 7.67, 3.50, 3.96, 5.71, 0.92, 0.59, and 1.69 ng mL?1, respectively. In short, the developed paper sensor is a useful tool for rapid and simple screening of residues of benzimidazoles in milk samples. 相似文献
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