633287-91-9Relevant academic research and scientific papers
Modification of biologically active amides and amines with fluorine-containing heterocycles 6. Methyl 3,3,3-trifluoro-2-(3-methyl-5-oxo-1- phenyl-1,5-dihydro-4H-pyrazol-4-ylidene)propionate in cyclocondensation with 1,3-binucleophiles
Sokolov,Aksinenko
, p. 1965 - 1968 (2013/12/04)
A reaction of methyl 3,3,3-trifluoro-2-(3-methyl-5-oxo-1-phenyl-1,5- dihydro-4H-pyrazol-4-ylidene)propionate with 1,3-binucleophiles (N-benzylurea, N-substituted 3-aminocrotonates, N-substituted 3-aminocyclohexenones, and 6-aminouracyls), leading to the formation of fluorine-containing heterocyclic 3-methyl-1-phenylpyrazol-5-one derivatives, was studied.
Synthesis and evaluation of a novel indoledione class of long chain fatty acid elongase 6 (ELOVL6) inhibitors
Takahashi, Toshiyuki,Nagase, Tsuyoshi,Sasaki, Takahide,Nagumo, Akira,Shimamura, Ken,Miyamoto, Yasuhisa,Kitazawa, Hidefumi,Kanesaka, Maki,Yoshimoto, Ryo,Aragane, Katsumi,Tokita, Shigeru,Sato, Nagaaki
supporting information; experimental part, p. 3142 - 3145 (2010/03/24)
Novel indoledione derivatives were synthesized and evaluated as long chain fatty acid elongase 6 (ELOVL6) inhibitors. Systematic optimization of an indole class of lead 1 led to the identification of potent ELOVL6 selective inhibitors. Representative inhibitor 37 showed sustained plasma exposure and good liver penetrability in mice. After oral administration, 37 potently inhibited ELOVL6 activity in the liver in mice.
