کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1399748 | 1501212 | 2008 | 11 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Syntheses of tetrahydroisoquinoline derivatives that inhibit NO production in activated BV-2 microglial cells Syntheses of tetrahydroisoquinoline derivatives that inhibit NO production in activated BV-2 microglial cells](/preview/png/1399748.png)
Seventeen tetrahydroisoquinoline derivatives were designed, synthesized and evaluated for inhibition of NO production in lipopolysaccharide-stimulated BV-2 microglial cells. Compounds 5a, 9c and 11a potently attenuated NO production by >60%, and 5a and 11a inhibited BH4 production by >48% at 100 μM. In particular, N-ethylcarbonyl-7-hydroxy-6-methoxy-1,2,3,4-tetrahydroisoquinoline (11a) reduced NO production by 64% and tetrahydrobiopterin (BH4) production by 49%. Introducing longer alkyl component at C1 or N2 position led to attenuation of the inhibitory effect. It is possible that 11a inhibits NO production by blocking BH4-dependent dimerization of newly synthesized iNOS monomers.
Seventeen tetrahydroisoquinoline derivatives have been synthesized and tested for their ability to inhibit NO synthesis.Figure optionsDownload as PowerPoint slide
Journal: European Journal of Medicinal Chemistry - Volume 43, Issue 6, June 2008, Pages 1160–1170