255060-81-2Relevant academic research and scientific papers
Highly potent inhibitors of TNF-α production. Part II: Metabolic stabilization of a newly found chemical lead and conformational analysis of an active diastereoisomer
Matsui, Toshiaki,Kondo, Takashi,Nishita, Yoshitaka,Itadani, Satoshi,Tsuruta, Hiroshi,Fujita, Setsuko,Omawari, Nagashige,Sakai, Masaru,Nakazawa, Shuichi,Ogata, Akihito,Mori, Hideaki,Kamoshima, Wataru,Terai, Kouichiro,Ohno, Hiroyuki,Obata, Takaaki,Nakai, Hisao,Toda, Masaaki
, p. 3787 - 3805 (2007/10/03)
Design and synthesis of metabolically stabilized inhibitors of TNF-α production, which could be new drug candidates, are reported. Conformational analysis of an active diastereoisomer was performed based on biological evaluations of the conformationally f
Synthesis of enantiomerically pure 2-amino alcohols from amino acids mediated by sulfoxides
Yuste, Francisco,Ortiz, Benjamin,Carrasco, Alejandra,Peralta, Martha,Quintero, Leticia,Sanchez-Obregon, Ruben,Walls, Fernando,Garcia Ruano, Jose L.
, p. 3079 - 3090 (2007/10/03)
Enantiomerically pure (R1,S2)- and (S1,S2)-2-amino alcohols can be easily synthesized by stereodivergent reduction of α'-(N-Boc)amino β-keto sulfoxides (easily synthesized from readily available N-Boc amino este
3-[3-(piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists
Russell, Michael G. N.,Matassa, Victor G.,Pengilley, Roy R.,Van Niel, Monique B.,Sohal, Bindi,Watt, Alan P.,Hitzel, Laure,Beer, Margaret S.,Stanton, Josephine A.,Broughton, Howard B.,Castro, José L.
, p. 4981 - 5001 (2007/10/03)
Several 5-HT(ID/1B) receptor agonists are now entering the marketplace as treatments for migraine. This paper describes the development of selective h5-HT(1D)receptor agonists as potential antimigraine agents which may produce fewer side effects. A series of 3-[3-(piperidin-1-yl)propyl]indoles has been synthesized which has led to the identification of 80 (L-772,405), a high- affinity h5-HT(1D) receptor full agonist having 170-fold selectivity for h5- HT(1D) receptors over h5-HT(1B) receptors. L-772,405 also shows very good selectivity over a range of other serotonin and nonserotonin receptors and has excellent bioavailability following subcutaneous administration in rats. It therefore constitutes a valuable tool to delineate the role of h5-HT(1D) receptors in migraine. Molecular modeling and physical properties have been utilized to postulate the binding conformation of these compounds in the receptor cavity.
