177755-69-0Relevant academic research and scientific papers
Discovery of novel spiro-piperidine derivatives as highly potent and selective melanin-concentrating hormone 1 receptor antagonists
Suzuki, Takao,Moriya, Minoru,Sakamoto, Toshihiro,Suga, Takuya,Kishino, Hiroyuki,Takahashi, Hidekazu,Ishikawa, Makoto,Nagai, Keita,Imai, Yumiko,Sekino, Etsuko,Ito, Masahiko,Iwaasa, Hisashi,Ishihara, Akane,Tokita, Shigeru,Kanatani, Akio,Sato, Nagaaki,Fukami, Takehiro
scheme or table, p. 3072 - 3077 (2010/02/28)
Optimization of high-throughput screening hit 1a led to the identification of a novel spiro-piperidine class of melanin-concentrating hormone 1 receptor (MCH-1R) antagonists. Compound 3c was identified as a highly potent and selective MCH-1R antagonist, which has an IC50 value of 0.09 nM at hMCH-1R. The synthesis and structure-activity relationships of the novel spiro-piperidine MCH-1R antagonists are described.
Benzenesulfonamide subtituted imidazolyl compounds for the treatment of inflammation
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, (2008/06/13)
A class of imidazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II STR1 wherein R1 is selected from lower alkyl, lower haloalkyl, lower hydroxyalkyl, lower aralkenyl, lower aryloxyalkyl, lower arylthioalkyl and heteroaryl; wherein R3 is selected from lower alkyl and amino; and wherein R4 is one or more radicals selected from hydrido, halo, lower alkyl and lower alkoxy; or where R4 together with the phenyl radical forms naphthyl or benzodioxolyl; provided R1 is not lower alkyl when R3 is methyl and when R4 is hydrido, methyl, methoxy or chloro; or a pharmaceutically-acceptable salt thereof.
