96306-54-6Relevant academic research and scientific papers
Synthesis of 1-(3,4-dihydroxy-5-nitrophenyl)-2-phenyl-ethanone and derivatives as potent and long-acting peripheral inhibitors of catechol-O-methyltransferase
Learmonth, David A.,Vieira-Coelho, Maria A.,Benes, Jan,Alves, Paula C.,Borges, Nuno,Freitas, Ana P.,Soares-da-Silva, Patrício
, p. 685 - 695 (2007/10/03)
A homologous series of novel nitro-catechol structures (7a-7e) were synthesized and tested as inhibitors of the enzyme catechol-O-methyltransferase (COMT). Increasing chain length was found to have significant impact on both brain penetration and duration
Agents for the treatment of overactive detrusor. IX. Synthesis and pharmacological properties of metabolites of N-tert-butyl-4,4-diphenyl-2- cyclopentenylamine (FK584) in human urine
Taniguchi, Kiyoshi,Miyao, Yasuhiro,Yamano, Katsuhiro,Yamamoto, Takao,Terai, Takao,Kusunoki, Takahiro,Tsubaki, Kazunori,Shiokawa, Youichi
, p. 1188 - 1195 (2007/10/03)
We synthesized the racemates of five presumed metabolites (1b-f) of (s)- (-)-N-tert-butyl-4,4-diphenyl-2-cyclopentenylamine hydrochloride (FK584, S(- )-1a), a novel agent for the treatment of overactive detrusor syndrome, in order to confirm the structures of the metabolites and also to evaluate their inhibitory activity against detrusor contraction. (±)-N-tert-Butyl-4-(4- hydroxyphenyl)- and 4-(4-hydroxy-3-methoxyphenyl)-4-phenyl-2-cyclopentenyl- amines (1b-e) were synthesized via 5-(4-methoxyphenyl)- and 5-(4-benzyloxy- 3-methoxyphenyl)-5-phenyl-2-cyclopenten-1-one (9g, h), respectively. Compounds 1b-f prepared in this study were identical with the metabolites in human urine in gas chromatography mass spectrometry and analytical HPLC. The inhibitory activity of compounds 1b-f against detrusor contraction in vitro induced by electrical field stimulation in guinea-pigs was less potent than that of FK584.
Metabolites of Cibenzoline: Synthesis of Hydroxylated 1,1-Diphenyl-2-imidazolylcyclopropanes and 5,5-Diphenyl-2H-pyrroloimidazolines
Tilley, Jefferson W.,Clader, John W.,Wirkus, Maria,Blount, John F.
, p. 2220 - 2224 (2007/10/02)
The (hydroxyphenyl)pyrroloimidazolines 7a and 7b, which are of interest as oxidative metabolites of the antiarrhythmic agent cibenzoline (1), were synthesized by the base-catalyzed rearrangement of the cyclopropylphenols derived from benzyl ethers
