107076-03-9Relevant academic research and scientific papers
Synthesis of metabolites of the cerebroprotecting agent 7-hydroxy-1- [[[4-(3-methoxyphenyl)-1-piperazinyl]acetyl]amino]-2,2,4,6-tetramethylindan (OPC-14117)
Otsubo, Kenji,Matsubara, Jun,Kitano, Kazuyoshi,Kawano, Yoshikazu,Ohtani, Tadaaki,Morita, Seiji,Sato, Seiji,Oshiro, Yasuo,Uchida, Minoru
, p. 728 - 732 (2007/10/03)
A hydroxylated metabolite (5a) of 7-hydroxy-1-[[[4-(3-methoxyphenyl)-1- piperazinyl]acetyl]amino]-2,2,4,6-tetramethylindan (OPC-14117), which is a novel cerebroprotective agent with central nervous system-stimulating activity, was synthesized by use of a model cytochrome P-450 system. In order to confirm the structure of this compound it was prepared by another route. The structures of several metabolites (5a, 7 and 8) were identified by means of comparisons with the synthetic compounds.
Synthesis and activity of 2-methyl-3-aminopropiophenones as centrally acting muscle relaxants
Shiozawa,Narita,Izumi,Kurashige,Sakitama,Ishikawa
, p. 85 - 94 (2007/10/02)
Some novel 2-methyl-3-aminopropiophenones were synthesized and their centrally acting muscle relaxant activities were,evaluated for an inhibitory effect on the flexor reflex in rats. The structure-activity relationships are discussed. In this series 2-methyl-3-pyrrolidino-1-(4-trifluoromethylphenyl)-propan-1-one (28) showed significant centrally acting muscle relaxant activity. In addition, the activities of each enantiomer (28-(S) and (R)) were studied along with their acute toxicities. Compound 28-(R) was found to exhibit more potent activity and weaker acute toxicity than 28-(S). Accordingly, compound 28-(R) (NK433) is under development as a novel centrally acting muscle relaxant.
