- Development of Quinazoline/Pyrimidine-2,4(1H,3H)-diones as Agonists of Cannabinoid Receptor Type 2
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Starting from a prototypical structure 1, we describe our efforts to design and obtain novel quinazoline/pyrimidine-2,4(1H,3H)-diones with high CB2 agonist potency and selectivity as well as improved physicochemical characteristics, mainly hydrophilicity. The most potent and selective CB2 agonists, 8 and 36, in this series were also endowed with lower logP values than that of GW842166X and lead compound 1. These derivatives appear to be promising lead compounds for the development of future CB2 agonists.
- Qian, Hai-Yan,Wang, Zhi-Long,Pan, You-Lu,Chen, Li-Li,Xie, Xin,Chen, Jian-Zhong
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supporting information
p. 678 - 681
(2017/06/13)
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- Quinazoline dione derivatives and preparation method and application thereof
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The invention provides novel quinazoline dione derivatives and a preparation method and application thereof. The compounds include compounds with the structure shown in the general formula V in the description and pharmaceutically acceptable salts or hydrates thereof. The compounds are active ligands of novel cannabinoid II receptors (CB2) and can be used for preparing medicine for treating, preventing and relieving CB2 receptor-mediated diseases, wherein the medicine is an agonist or partial agonist or inverse agonist or antagonist of CB2 receptors.
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Paragraph 0445; 0446; 0447
(2017/07/19)
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- Synthesis of 1-substituted 4(1H)-quinazolinones under solvent-free conditions
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(Chemical Equation Presented) Heating a mixture of 2-(N-alkylamino)benzoic acids, triethyl orthoformate, and ammonium acetate under solvent-free conditions generated 1-substituted 4(1H)- quinazolinones in 73-99% yields. Moreover, a possible reaction pathway was proposed. Copyright Taylor & Francis Group, LLC.
- Wang, Yao,Zhang, Mei,Cao, Shengli,Lin, Huihui,Gao, Man,Li, Zhongfeng
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p. 2715 - 2727
(2012/07/14)
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- Efficient copper-catalyzed synthesis of N-alkylanthranilic acids via an ortho-substituent effect of the carboxyl group of 2-halobenzoic acids at room temperature
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We have developed an efficient copper-catalyzed method for the synthesis of N-alkylanthranilic acids. The protocol uses inexpensive copper(I) iodide/racemic 1,1'-binaphthyl-2,2'-diol (rac-BINOL) as the catalyst/ligand system, readily available 2-halobenzoic acids and aliphatic amines as the starting materials, the coupling reactions were performed at room temperature, and various functionalities in the substrates were tolerated.
- Zeng, Liang,Fu, Hua,Qiao, Renzhong,Jiang, Yuyang,Zhao, Yufen
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supporting information; experimental part
p. 1671 - 1676
(2011/02/25)
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- A simple and efficient approach to quinazolinones under mild copper-catalyzed conditions
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(Chemical Equation Presented) Cop some rings: A simple and highly efficient copper-catalyzed method for the synthesis of quinazolinone derivatives through the reaction of substituted 2-halobenzoic acids with amidines or guanidines under mild conditions ha
- Liu, Xiaowei,Fu, Hua,Jiang, Yuyang,Zhao, Yufen
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supporting information; experimental part
p. 348 - 351
(2009/04/14)
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