- 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; 0454; 0455
(2017/07/19)
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- Ultrasound-promoted reaction of 2-chlorobenzoic acids and aliphatic amines
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An improvement to the use of DMF as a solvent for the condensation of 2-chlorobenzoic acids with aliphatic primary or secondary amines was described. A number of alkylaminobenzoic acids and dialkylaminobenzoic acids were synthesized in acceptable-to-good yield. The advantages of this procedure include readily available substrates, the use of an inexpensive copper powder without taking any precautions to exclude moisture under mild conditions and experimental ease. Furthermore, this condensation could also be achieved under nonclassical conditions by using ultrasonic irradiation at room temperature. We demonstrated that ultrasound-promoted condensation of 2-chlorobenzoic acid with aliphatic amines with the use of DMF as the solvent, especially in the case of secondary amines, affords products in high yields and reduces the reaction time to minutes. The results proved to be highly reproducible because the relevant sonochemical parameters were rigorously controlled. Wiley-VCH Verlag GmbH & Co. KGaA, 2007.
- Docampo, Maite L.,Pellon, Rolando F.,Estevez-Braun, Ana,Ravelo, Angel G.
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p. 4111 - 4115
(2008/02/13)
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- Use of ultrasound in the synthesis of 2-(alkylamino)benzoic acids in water
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The synthesis of substituted 2-(alkylamino)benzoic acids using the Ullmann condensation with water as the solvent and utilizing ultrasound irradiation was achieved with high yields in a short reaction time. Georg Thieme Verlag Stuttgart.
- Pellón, Rolando F.,Estévez-Braun, Ana,Docampo, Maite L.,Martín, Ana,Ravelo, Angel G.
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p. 1606 - 1608
(2007/10/03)
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