基于结构-活性关系 乙恶唑设计并合成了一系列的2-(2,6-二氟苯基)-4-(4-取代的苯基)-1,3-恶唑啉4a-y和苯甲酰基苯基脲。发现大多数这些化合物显示出优异的杀螨活性。当浓度为2.5 mg L -1时,它们对蜘蛛螨的卵和幼虫的死亡率都达到85%以上。一些化合物还表现出优异的杀虫活性。2,4-二苯基-1,3-恶唑啉的4-苯基上的取代基的位置和类型对活性有很大影响。2-(2,6-二氟苯基)-4-(2-Cl-4-(4-Cl-苯氧基)苯基)-1,3-恶唑啉(4r)在2.5 mg L -1下表现出100%的杀螨作用,对甜菜夜蛾和小菜蛾的死亡率分别为12.5 mg L -1和65%和93%,几乎与乙恶唑。新发现的结构-活性关系也可能有益于进一步的杀螨剂/杀虫剂开发。
Aryl ethers can be constructed from the direct coupling between the benzene C–H bond and the alcohol O–H bond with the evolution of hydrogen via the synergistic merger of photocatalysis and cobalt catalysis. Utilizing the dual catalyst system consisting of 3-cyano-1-methylquinolinum photocatalyst and cobaloxime, intermolecular etherification of arenes with various alcohols and intramolecular alkoxylation
Keratinocyte growth inhibitors and hydroxamic acid derivatives
申请人:——
公开号:US20030229113A1
公开(公告)日:2003-12-11
This invention relates to a keratinocyte-proliferation inhibitor comprising as active ingredient a compound having an activity of inhibiting the solubilization of heparin-binding EGF-like growth factor bound to cell membranes and a compound of the formula (I);
1
or pharmaceutically acceptable salt thereof, wherein R
1
, R
2
, R
3
are hydrogen atom or alkyl and X is substituted benzene or the like.
Novel Fluorinated Derivatives of the Broad-Spectrum MMP Inhibitors <i>N</i>-Hydroxy-2(<i>R</i>)-[[(4-methoxyphenyl)sulfonyl](benzyl)- and (3-picolyl)-amino]-3-methyl-butanamide as Potential Tools for the Molecular Imaging of Activated MMPs with PET
An approach to the in vivo imaging of locally upregulated and activated matrix metalloproteinases (MMPs) found in many pathological processes is offered by positron emission tomography (PET). Hence, appropriate PET radioligands for MMP imaging are required. Here, we describe the syntheses of novel fluorinated MMP inhibitors (MMPIs) based on lead structures of the broad-spectrum inhibitors N-hydrox
A Product Analytical Study of the Thermal and Photolytic Decomposition of Some Arenediazonium Salts in Solution
作者:Peter S. J. Canning、Howard Maskill、Katharine McCrudden、Brian Sexton
DOI:10.1246/bcsj.75.789
日期:2002.4
most solvents undergo unimolecular heterolysis to give singlet aryl cations which are captured by solvent. This mechanism is dominant for arenediazonium ions without electron-withdrawing substituents in all solvents, and the only reaction observed in water. Additionally, appreciable yields of fluoroarenes are obtained by fluoride abstraction by the aryl cation from fluorinated solvents and from tetrafluoroborate
DERIVATIVES OF 4-(2-AMINO-1-HYDROXYETHYL)PHENOL AS AGONISTS OF THE BETA2 ADRENERGIC RECEPTOR
申请人:Tanã Jordi Bach
公开号:US20100168161A1
公开(公告)日:2010-07-01
The present relates to compounds of formula (I):
or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof. The present disclosure also relates to pharmaceutical compositions comprising the compounds of formula (I), and to their methods of use in therapy.