112798-58-0Relevant academic research and scientific papers
Syntheses of NAMDA derivatives inhibiting NO production in BV-2 cells stimulated with lipopolysaccharide
Jai, Woong Seo,Srisook, Ekaruth,Hyo, Jin Son,Hwang, Onyou,Cha, Young-Nam,Dae, Yoon Chi
, p. 3369 - 3373 (2007/10/03)
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.
Synthesis of N,N′,N″-trisubstituted thiourea derivatives and their antagonist effect on the vanilloid receptor
Park, Hyeung-Geun,Park, Mi-Kyung,Choi, Ji-Yeon,Choi, Sea-Hoon,Lee, Jihye,Park, Boon-Saeng,Kim, Myoung Goo,Suh, Young-Ger,Cho, Hawon,Oh, Uhtaek,Lee, Jeewoo,Kim, Hee-Doo,Park, Young-Ho,Koh, Hyun-Ju,Lim, Kyung Min,Moh, Joo-Hyun,Jew, Sang-Sup
, p. 601 - 604 (2007/10/03)
Twenty-seven N,N′,N″-trisubstituted thiourea derivatives were prepared. Among them, 1-[3-(4′-hydroxy-3′-methoxy-phenyl)-propyl]-1,3-diphenethyl- thiourea (8l, IC50=0.32 μM), showed 2-fold higher antagonistic activity than that of capsazepine (3
Iodine (III)-mediated generation of nitrogen-tethered orthoquinol acetates for the construction of oxygenated indole, quinoline, and phenanthridine alkaloid motifs
Pouysegu, Laurent,Avellan, Anne-Virginie,Quideau, Stephane
, p. 3425 - 3436 (2007/10/03)
Functionalized indole and quinoline derivatives are conveniently prepared from nitrogen-tethered 2-methoxyphenols via phenyliodine(III) diacetate mediated oxidative acetoxylation, followed by a fluoride- or base-induced intramolecular nucleophilic addition reaction. This regioselective Michael-type addition step is further discussed in view of the rearrangement of orthoquinol acetate intermediates into paraquinol acetates that is sometimes observed in situ. Application of this methodology to the synthesis of a functionalized phenanthridine, and its potential for the construction of polyoxygenated lycorine-type alkaloid skeleta are here described.
