2396-17-0Relevant articles and documents
Polyfluoroalkyl-containing isoindolinone benzamide derivative, preparation method and application thereof
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Paragraph 0111-0115, (2021/05/12)
The invention provides a polyfluoroalkyl-containing isoindolinone benzamide derivative, which has the following general formula A-1 as shown in the specification, wherein substituent groups are shown as the specification. The polyfluoroalkyl-containing isoindolinone benzamide derivative provided by the invention is suitable for agricultural insecticide.
METHOD FOR PRODUCING SUBSTITUTED N-ARYL PYRAZOLES
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Paragraph 0311; 0312, (2021/09/10)
The present invention relates to a process for preparing compounds of the formula (I) starting from compounds of the formula (II) in which R1, R2 and R3 have the abovementioned meaning and where R1 and R3
Discovery of tetrahydroquinolines and benzomorpholines as novel potent RORγt agonists
Xia, Yuehan,Yu, Mingcheng,Zhao, Yunpeng,Xia, Li,Huang, Yafei,Sun, Nannan,Song, Meiqi,Guo, Huimin,Zhang, Yunyi,Zhu, Di,Xie, Qiong,Wang, Yonghui
supporting information, (2020/12/04)
The retinoic acid receptor-related orphan receptor γt (RORγt) is an important nuclear receptor that regulates the differentiation of Th17 cells and production of interleukin 17(IL-17). RORγt agonists increase basal activity of RORγt and could provide a potential approach to cancer immunotherapy. Herein, hit compound 1 was identified as a weak RORγt agonist during in-house library screening. Changes in LHS core of 1 led to the identification of tetrahydroquinoline compound 6 as a partial RORγt agonist (max. act. = 39.3%). Detailed structure-activity relationship on substituent of the LHS core, amide linker and RHS arylsulfonyl moiety was explored and a novel series of tetrahydroquinolines and benzomorpholines was discovered as potent RORγt agonists. Tetrahydroquinoline compound 8g (EC50 = 8.9 ± 0.4 nM, max. act. = 104.5%) and benzomorpholine compound 9g (EC50 = 7.5 ± 0.6 nM, max. act. = 105.8%) were representative compounds with high RORγt agonistic activity in dual FRET assay, and they showed good activity in cell-based Gal4 reporter gene assay and Th17 cell differentiation assay (104.5% activation at 300 nM of 8g; 59.4% activation at 300 nM of 9g). The binding modes of 8g and 9g as well as the two RORγt inverse agonists accidentally discovered were also discussed.
Synthetic method of pyridine quinazoline intermediate
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Paragraph 0009; 0012; 0016; 0020; 0024, (2020/08/25)
The invention discloses a synthesis method of a pyridine quinazoline intermediate, which comprises the following steps: by using nitrobenzene as an initial raw material, carrying out a nitro reductionreaction, a benzene ring substitution reaction, an amino protection reaction, a chloromethylation reaction and a hydrazine hydrate cyclization reaction to obtain 3-amino-6-(perfluoropropane-2-yl)-3,4-dihydroquinazoline-2(1H)-ketone. The nitrobenzene is adopted as a starting material, benzene ring nitro reduction and benzene ring substitution reaction are achieved through a one-pot method, meanwhile, the nitrobenzene inhibits generation of fluorine-removed impurities in the benzene ring substitution reaction, the synthesis process is simplified, and the yield is increased. The chloromethylation reaction avoids the problems of many benzyl chloride impurities, strong smell, high risk and the like in the traditional route, enhances the yield, and implements the environment friendliness of thesynthesis technique. The method is simple in technological operation, low in raw material cost, environmentally friendly and suitable for large-scale production.
Synthesis and fungicidal activities of perfluoropropan-2-yl-based novel quinoline derivatives
Zhang, Zai,Liu, Minhua,Liu, Weidong,Xiang, Jun,Li, Jianming,Li, Zhong,Liu, Xingping,Huang, Mingzhi,Liu, Aiping,Zheng, Xingliang
, p. 91 - 97 (2019/06/24)
A series of novel perfluoropropan-2-yl-based quinoline derivatives was designed and synthesized utilizing tebufloquin as the lead compound. The structures of all the newly synthesized compounds were confirmed by spectroscopic data 1HNMR, MS and elemental analysis. The results of bioassay indicated that these compounds exhibited potent fungicidal activities against Erysiphe graminis. Especially, compound 8c displayed excellent activity with EC50 value at 1.48 mg / L, which was better than that of the commercialized fungicide-tebufloquin. The structure-activity relationship for these new compounds was also discussed.
Metabolism study and biological evaluation of bosentan derivatives
Lepri, Susan,Goracci, Laura,Valeri, Aurora,Cruciani, Gabriele
, p. 658 - 670 (2016/07/06)
Bosentan, the first-in-class drug used in treatment of pulmonary arterial hypertension, is principally metabolized by the cytochromes P450, and it is responsible for cytochromes induction and drug-drug interaction events with moderate to severe consequences. A strategy to reduce drug-drug interactions consists of increasing the metabolic stability of the perpetrator, and fluorinated analogues are often designed to block the major sites of metabolism. In this paper bosentan analogues were synthesized, and their metabolism and biological activity were evaluated. All synthesized compounds showed an improved metabolic stability towards CYP2C9, with one maintaining a moderate antagonist effect towards the ETA receptor.
Synthesis, insecticidal activities and SAR of novel phthalamides targeting calcium channel
Chen, Youwei,Li, Yuxin,Pan, Li,Liu, Jingbo,Wan, Yingying,Chen, Wei,Xiong, Lixia,Yang, Na,Song, Haibin,Li, Zhengming
, p. 6366 - 6379 (2015/01/09)
In order to find novel and environmental friendly insecticides targeting the ryanodine receptor, three series of novel phthalamides containing heptafluoroisopropyl group, low fluorine atoms group and non-fluorine group were designed and synthesized. 35 novel structures of three series were obtained. Insecticidal activities of title compounds against oriental armyworm (Mythimna separata) and diamondback moth (Plutella xylostella) indicated that most of title compounds showed moderate to high activities at the tested concentration. The structure-activity relationship (SAR) was discussed in detail. During synthesizing title compounds B8, C7, D1, D9 and D12, their corresponding positional isomers (B8′, C7′, D1′, D9′ and D12′) were afforded, and their structures were confirmed by 2D NMR. The calcium-imaging technique was also applied to investigate the effects of compounds B2, B10, C4 and C5 on the intracellular calcium ion concentration ([Ca2+]i), which indicated that they released stored calcium ions from endoplasmic reticulum, which denoted that some compounds are potential modulators of the insect ryanodine receptor (RyR).
Optimized inhibitors of soluble epoxide hydrolase improve in vitro target residence time and in vivo efficacy
Lee, Kin Sing Stephen,Liu, Jun-Yan,Wagner, Karen M.,Pakhomova, Svetlana,Dong, Hua,Morisseau, Christophe,Fu, Samuel H.,Yang, Jun,Wang, Peng,Ulu, Arzu,Mate, Christina A.,Nguyen, Long V.,Hwang, Sung Hee,Edin, Matthew L.,Mara, Alexandria A.,Wulff, Heike,Newcomer, Marcia E.,Zeldin, Darryl C.,Hammock, Bruce D.
supporting information, p. 7016 - 7030 (2014/11/07)
Diabetes is affecting the life of millions of people. A large proportion of diabetic patients suffer from severe complications such as neuropathic pain, and current treatments for these complications have deleterious side effects. Thus, alternate therapeu
AMIDE DERIVATIVE, PEST CONTROL AGENT CONTAINING THE AMIDE DERIVATIVE AND USE OF THE PEST CONTROL AGENT
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Page/Page column 330, (2011/05/14)
An amide derivative represented by the following Formula (1) is provided as an amide derivative showing a significantly excellent effect for a pest control action. In the following Formula (1), A represents a carbon atom, a nitrogen atom, or the like, and K represents a non-metal atomic group necessary for forming a cyclic linking group derived from benzene or a heterocyclie. X represents a halogen atom or the like; n represents an integer of from 0 to 4. R1 and R2 represent hydrogen atoms, alkyl groups, or the like. T represents -C(=G1)-Q1 or -C(=G1)-G2Q2, and G1 to G3 each represent oxygen atoms or the like. Q1 and Q2 each represent a hydrogen atom, an alkyl group, an aryl group, or the like. Y1 and Y5 each represent a halogen atom or the like, Y2 and Y4 each represent a hydrogen atom or the like, and Y3 represents a C2-C5 haloalkyl group.
AMIDE DERIVATIVE, PEST CONTROL AGENT CONTAINING THE AMIDE DERIVATIVE AND PEST CONTROLLING METHOD
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Page/Page column 452, (2011/06/24)
A pest control agent containing a compound represented by the following Formula (1), wherein A represents a carbon atom, a nitrogen atom, or the like, K represents a non-metal atom group necessary for forming a cyclic linking group derived from a 5- or 6-membered aromatic ring, in combination with A and two carbon atoms to which A bonds, X represents a hydrogen atom, a halogen atom, or the like, n represents an integer of from 0 to 4, T represents -C(=G1)-Q1 (wherein G1 and G2 represent an oxygen atom or the like, Q1 represents a phenyl group which may have a substituent, a heterocyclic group which may have a substituent, or the like), or the like, Q2 represents a phenyl group or the like, G3 represents an oxygen atom or the like, and R1 and R2 each independently represent a hydrogen atom, a C1-C6 alkyl group, or a group represented by -L-D, or the like (provided that at least either R1 or R2 represents a group represented by -L-D); as an active ingredient exhibits an excellent effect.
