152911-39-2Relevant academic research and scientific papers
Identification of N-{[6-chloro-4-(2,6-dimethoxyphenyl)quinazolin-2-yl]carbonyl}-l-leucine (NTRC-808), a novel nonpeptide chemotype selective for the neurotensin receptor type 2
Thomas, James B.,Giddings, Angela M.,Olepu, Srinivas,Wiethe, Robert W.,Harris, Danni L.,Narayanan, Sanju,Warner, Keith R.,Sarret, Philippe,Longpre, Jean-Michel,Runyon, Scott P.,Gilmour, Brian P.
, p. 292 - 296 (2015)
Compounds acting via the GPCR neurotensin receptor type 2 (NTS2) display analgesic effects in relevant animal models. Using a pharmacophore model based on known NT receptor nonpeptide compounds, we screened commercial databases to identify compounds that
Novel 4,1-benzoxazepine derivatives with potent squalene synthase inhibitory activities
Miki, Takashi,Kori, Masakuni,Mabuchi, Hiroshi,Banno, Hiroshi,Tozawa, Ryu-ichi,Nakamura, Masahira,Itokawa, Shigekazu,Sugiyama, Yasuo,Yukimasa, Hidefumi
, p. 401 - 414 (2007/10/03)
A series of (3,5-trans)-2-oxo-5-phenyl-1,2,3,5-tetrahydro-4,1-benzoxazepine derivatives were synthesized and evaluated for squalene synthase inhibitory and cholesterol biosynthesis inhibitory activities. Through modification of substituents of the lead compounds 1a and 1b, it was found that 4,1-benzoxazepine-3-acetic acid derivatives with isobutyl and neopentyl groups at the 1-position, the chloro atom at the 7-position, and the chloro and methoxy groups at the 2'-position on the 5-phenyl ring, had potent squalene synthase inhibitory activity. Among such compounds, the 5-(2,3-dimethoxyphenyl) derivative 2t exhibited potent inhibition of cholesterol biosynthesis in HepG2 cells. As a result of optical resolution study of 2t, the absolute stereochemistry required for inibitory activity was determined to be 3R,5S. In vivo study showed that the sodium salt of (3R,5S)-7-chloro-5-(2,3-dimethoxyphenyl)-1-neopentyl-2-oxo-1,2,3,5-tetrahydro-4,1-benzoxazepine-3-aceitc acid 20 effectively reduced plasma cholesterol in marmosets. Copyright
