- Synthesis of 1,8-naphthyridine derivatives: Potential antihypertensive agents - Part VII
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A series of 2-(carbethoxypiperazinyl)- and 2-piperazinyl-1,8- naphthyridine derivatives, variously substituted, have been synthesized and pharmacologically investigated for their antihypertensive activity. Some of them exhibited a significant and prolonged decrease of the mean arterial pressure (MAP) on spontaneously hypertensive rats. For this series of compounds, on the basis of the pharmacological results obtained, no structure-activity relationship can be deduced at this time. Moreover, the most active and representative compounds 11b, 12a and 16b were investigated by means of in vitro pharmacological functional studies and in vivo, as diuretic agents, to determine a possible mechanism of the antihypertensive activity, which is unknown for the moment.
- Ferrarini, Pier Luigi,Mori, Claudio,Badawneh, Muwaffag,Calderone, Vincenzo,Calzolari, Lorella,Loffredo, Tiziana,Martinotti, Enrica,Saccomanni, Giuseppe
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- COMPOUNDS AND METHODS FOR INHIBITING mTOR
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Compounds having activity as mTOR inhibitors are disclosed. The compounds have the following structure (I) including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4, and A are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
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(2017/03/14)
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- Substituted 1,8-naphthyridines, their preparation and their use as antidotes
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A combination of a variety of herbicides with safening agents which are substituted 1,8-naphthyridines of the formula STR1 where R1 is mercapto, hydroxyl, halogen, benzylthio, amino or NR2 R3, where R2 is a grou
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