设计,合成了一系列含有卤素,三氟甲基和氰基的新型邻氨基苯甲酰胺衍生物(7a–s),并通过熔点,1 H NMR,13 C NMR和元素分析对其进行了表征。生物活性表明,它们中的大多数对东方粘虫(Mythimna separata)和小菜蛾(Plutella xylostella)表现出中等至优异的活性。首先,的杀幼虫活性70对粘虫率为100%,为0.25的40%和0.1毫克的L -1,比得上标准氯虫苯甲酰胺(100%,0.25毫克的L的-1和20%,0.1毫克的L - 1)。更,对抗小菜蛾的7o在0.01 mg L -1时显示出90%的杀虫活性,优于四氯苯丙胺(45%,0.01 mg L -1)。将美国蟑螂(Periplaneta Americana)心脏跳动率(背血管)和收缩力的实验7o与绿头兰醇进行了比较。此外,7o可能会影响东方粘虫第三幼虫中枢神经元的钙稳态,这表明,ryanodine
Photopharmacology develops bioactive compounds whose pharmacological potency can be regulated by light. The concept relies on the introduction of molecular photoswitches, such as azobenzenes, into the structure of bioactive compounds, such as known enzyme inhibitors. Until now, the development of photocontrolled protein kinase inhibitors proved to be challenging for photopharmacology. Here, we describe
Molecules having pesticidal utility, and intermediates, compositions, and processes, related thereto
申请人:Dow AgroSciences LLC
公开号:US20180279612A1
公开(公告)日:2018-10-04
This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).
Synthesis and Biological Study of 3-Butyl-1-(2,6-dichlorophenyl)-1H-[1,2,4]triazol- 5(4H)-one Derivatives as Anti-hypertension Drugs
作者:Yanchun Zhang、Jinpei Zhou、Weihong Pan、Xiaoming Wu、Shuai Wang
DOI:10.2174/157018010789869370
日期:2010.1.1
A series of nitric oxide-donating derivatives of [1,2,4]triazol-5(4H)-one (9a-f and 15a-f) as a novel class of angiotensin II receptor AT1 antagonists have been designed and synthesized by coupling furoxan and nitric oxide with lead compound 1. The synthesized compounds were evaluated for their antagonism of AT1 receptor with induced contraction in the rabbit thoracic aortic ring and the results showed that compounds 9b, 15b and 15d exhibited potent antagonistic activity of AT1 receptor. Moreover 9b, 15b, 15d, 15e had good maximum NO release amount of this series.
[EN] COMPOUNDS AND METHODS FOR MODULATING FXR<br/>[FR] COMPOSÉS ET PROCÉDÉS POUR MODULER LE FXR
申请人:LILLY CO ELI
公开号:WO2009012125A1
公开(公告)日:2009-01-22
Compounds of formula (I): formula (I) wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and diseases related to dyslipidemia.
Synthesis and Biological Evaluation of Benzimidazole Phenylhydrazone Derivatives as Antifungal Agents against Phytopathogenic Fungi
作者:Xing Wang、Yong-Fei Chen、Wei Yan、Ling-Ling Cao、Yong-Hao Ye
DOI:10.3390/molecules21111574
日期:——
A series of benzimidazole phenylhydrazone derivatives (6a-6ai) were synthesized and characterized by ¹H-NMR, ESI-MS, and elemental analysis. The structure of 6b was further confirmed by single crystal X-ray diffraction as (E)-configuration. All the compounds were screened for antifungal activity against Rhizoctonia solani and Magnaporthe oryzae employing a mycelium growth rate method. Compound 6f exhibited