- Synthesis and biological evaluation of novel hybrid chalcone derivatives as vasorelaxant agents
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With the aim to further improve the vasorelaxant activities of chalcones, nine hybrid chalcone derivatives conjugated with nitric oxide (NO) donor or 1,4-dihydropyridyl (1,4-DHP) moiety were designed and synthesized based on molecular hybridization strategy. Their vasorelaxant activities were evaluated in aortic rings with endothelium pre-contracted with phenylephrine (PE). All of these compounds showed preferable vasorelaxant activities which were more potent than their parent compounds. Compounds 8c and 15c, the most potent compounds, would be promising structural templates for the development of novel vasorelaxant agents. Nine hybrid chalcone derivatives conjugated with nitric oxide (NO) donors or 1,4-dihydropyridyl moiety were designed, synthesized and biological evaluated for their vasorelaxant activities.
- Dong, Xiaowu,Du, Lilin,Pan, Zhichao,Liu, Tao,Yang, Bo,Hu, Yongzhou
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scheme or table
p. 3986 - 3992
(2010/09/14)
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- Pharmacochemistry of the furoxan ring: Recent developments
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In the present work recent results obtained in the pharmacochemistry of the furoxan system are reported. In particular, after a brief description of the salient points of the furoxan chemistry, the synthesis and the properties of a series of Nifedipine and Prazosin analogues, containing this heterocyclic system, are described. Since we observed that a few furoxan derivatives are able to elicit both a dose-dependent rise in platelet cGMP levels and to promote a dose-dependent inhibition of AA-induced [Ca++] rise, and that many substituted furoxans show potent vasodilating and antiaggregatory activity, the possibility of using the furoxan system as a lead in the design of new vasodilators is also discussed.
- Calvino,Di Stilo,Fruttero,Gasco,Sorba,Gasco
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p. 321 - 334
(2007/10/02)
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- Unsymmetrically Substituted Furoxans. Part 11. Methylfuroxancarbaldehydes
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The two isomeric 3-methyl-4-furoxancarbaldehydes (2a) and 4-methyl-3-furoxancarbaldehyde (2b) have been prepared.Discussion of their structures, thermal equilibration and kinetic of thermal conversion from the 3-methyl to the 4-methyl isomer are also repo
- Fruttero, Roberta,Ferrarotti, Bruno,Serafino, Anna,Stilo, Antonella Di,Gasco, Alberto
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p. 1345 - 1347
(2007/10/02)
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