- Synthesis of novel ethyl 2,4-disubstituted 8-(trifluoromethyl)pyrido[2',3':3,4]pyrazolo[1,5-a]pyrimidine-9-carboxylate derivatives as promising anticancer agents
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A series of novel pyrido[2',3':3,4] pyrazolo[1,5-a]pyrimidine derivatives 6–9 were prepared in single step starting from 3-amino-6-(trifluoromethyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxylate 5 on reaction with symmetrical and unsymmetrical aliphatic and ar
- Ravi Kumar,Poornachandra,Krishna Swaroop,Jitender Dev,Ganesh Kumar,Narsaiah
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- A novel series of piperazinyl-pyridine ureas as antagonists of the purinergic P2Y12 receptor
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A novel series of P2Y12 antagonists for development of drugs within the antiplatelet area is presented. The synthesis of the piperazinyl-pyridine urea derivatives and their structure-activity relationships (SAR) are described. Several compounds
- Bach, Peter,Bostr?m, Jonas,Brickmann, Kay,Van Giezen,Hovland, Ragnar,Petersson, Annika U.,Ray, Asim,Zetterberg, Fredrik
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p. 2877 - 2881
(2011/06/24)
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- Synthesis and cardiotonic activity of 2-substituted 5-cyano-1,6-dihydro-6-oxo-3-pyridinecarboxylic acids and their methyl or ethyl esters
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The synthesis of ethyl or methyl esters of 5-cyano-1,6-dihydro-6-oxo-3-pyridinecarboxylic acids carrying as 2-substituent a polar group such as CO2C2H5, (CH2)2CO2CH3, (CH2)3CO2C2H5, CH2OCH3, or CF3 group is described. Also 2-[5-cyano-1,6-dihydro-2-(1,1-dimethylethyl)-6-oxo-3-pyridyl]-2-oxoace tic acid and 2,5,6,8-tetrahydro-2,5-dioxo-1H-thiopyrano[3,4-b]pyridine-3-carbonitri le were prepared. Nearly all the above esters gave routinely the corresponding carboxylic acids by alkaline hydrolysis followed by acidification. As milrinone analogues, the above compounds were tested on contractile activity and frequency rate of spontaneously beating atria from reserpine-treated guinea-pigs. 5-Cyano-2-trifuoromethyl-1,6-dihydro-6-oxo-3-pyridinecarboxylic acid and, in a lesser degree, the relative ethyl ester showed an appreciable positive inotropic activity, although inferior to that of milrinone.
- Mosti,Menozzi,Schenone,Dorigo,Gaion,Belluco
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p. 427 - 437
(2007/10/02)
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