- Syntheses of NAMDA derivatives inhibiting NO production in BV-2 cells stimulated with lipopolysaccharide
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Sixteen derivatives of N-acetyl-3-O-methyldopamine (NAMDA), an inhibitor of BH4 synthesis, were designed and synthesized. The ability of these derivatives to inhibit NO and BH4 production by lipopolysaccharide- stimulated BV-2 microglial cells was determined. While NAMDA at 100 μM inhibited NO and BH4 production by only about 20%, its catecholamide 8, indole 23 derivative, 13, and N-acetyl tetrahydroisoquinoline 25 inhibited the NO production by >50% at the same concentration. In particular, 13 and 25 inhibited both NO and BH4 production to similar degrees, which suggested that these compounds might inhibit NO production by blocking BH 4-dependent dimerization of the newly synthesized iNOS monomer.
- Jai, Woong Seo,Srisook, Ekaruth,Hyo, Jin Son,Hwang, Onyou,Cha, Young-Nam,Dae, Yoon Chi
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p. 3369 - 3373
(2007/10/03)
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- NEUROPROTECTIVE COMPOUNDS AND USES THEREOF
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The present invention relates to a compound having the formula: where X=R1O, F, Br, I, Cl, or a C1 to C5 alkyl group, R1=a C1 to C10 alkyl group or a C1 to C10 aryl group, n=1 or 2, R2=a C1 to C6 alkyl group, an amino acid, a heterocycle, a secondary or tertiary C3 to C4 hydrocarbon, or where R3=H or CH3, or pharmaceutically-acceptable salts thereof. The invention further relates to pharmaceutical compositions which include the compounds, as well as methods of making and using the compounds.
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