913624-97-2Relevant academic research and scientific papers
MMPL3 INHIBITORS, COMPOSITIONS AND USES THEREOF
-
Paragraph 0203; 0205, (2020/06/10)
Disclosed are inhibitors of mycobacterial membrane protein MmpL3, compositions comprising the inhibitors, and methods of preparation and use thereof.
Novel pyrazole derivatives as neutral CB1 antagonists with significant activity towards food intake
Manca, Ilaria,Mastinu, Andrea,Olimpieri, Francesca,Falzoi, Matteo,Sani, Monica,Ruiu, Stefania,Loriga, Giovanni,Volonterio, Alessandro,Tambaro, Simone,Bottazzi, Mirko Emilio Heiner,Zanda, Matteo,Pinna, Gerard Aime,Lazzari, Paolo
, p. 256 - 269 (2013/06/26)
In spite of rimonabant's withdrawal from the European market due to its adverse effects, interest in the development of drugs based on CB1 antagonists is revamping on the basis of the peculiar properties of this class of compounds. In particular, new strategies have been proposed for the treatment of obesity and/or related risk factors through CB1 antagonists, i.e. by the development of selectively peripherally acting agents or by the identification of neutral CB1 antagonists. New compounds based on the lead CB1 antagonist/inverse agonist rimonabant have been synthesized with focus on obtaining neutral CB1 antagonists. Amongst the new derivatives described in this paper, the mixture of the two enantiomers (±)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-(2-cyclohexyl-1- hydroxyethyl)-4-methyl-1H-pyrazole ((±)-5), and compound 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-[(Z)-2-cyclohexyl-1-fluorovinyl] -4-methyl-1H-pyrazole ((Z)-6), showed interesting pharmacological profiles. According to the preliminary pharmacological evaluation, these novel pyrazole derivatives showed in fact both neutral CB1 antagonism behaviour and significant in vivo activity towards food intake.
Design, synthesis and biological evaluation of CB1 cannabinoid receptor ligands derived from the 1,5-diarylpyrazole scaffold
Tu, Guogang,Xiong, Fang,Huang, Huiming,Kuang, Binhai,Li, Shaohua
experimental part, p. 222 - 230 (2011/11/06)
The CB1 receptor belongs to the G-protein-coupled receptor superfamily. CB1 antagonism has been considered as a new therapeutic target for the treatment of obesity. In this study, we report the synthesis and in vitro binding affinity assay of some 1,5-dia
1,5-DIARYL-PYRAZOLES AND THEIR USE AS CANNABINOID RECEPTOR NEUTRAL ANTAGONISTS
-
Page/Page column 41; 60-61, (2010/04/03)
The present invention pertains to cannabinoid (CB) receptor and cannabinoid-like receptor neutral antagonists, and especially CB1 neutral antagonists of Formula (I). The present invention also pertains to these compounds for use in the treatment of diseas
Discovery of novel arylpyrazole series as potent and selective opioid receptor-like 1 (ORL1) antagonists
Kobayashi, Kensuke,Uchiyama, Minaho,Ito, Hirokatsu,Takahashi, Hirobumi,Yoshizumi, Takashi,Sakoh, Hiroki,Nagatomi, Yasushi,Asai, Masanori,Miyazoe, Hiroshi,Tsujita, Tomohiro,Hirayama, Mioko,Ozaki, Satoshi,Tani, Takeshi,Ishii, Yasuyuki,Ohta, Hisashi,Okamoto, Osamu
scheme or table, p. 3627 - 3631 (2010/08/06)
The synthesis and biological evaluation of new potent opioid receptor-like 1 antagonists are presented. A structure-activity relationship (SAR) study of arylpyrazole lead compound 1 obtained from library screening identified compound 31, (1S,3R)-N-{[1-(3-
Biarylpyrazole inverse agonists at the cannabinoid CB1 receptor: Importance of the C-3 carboxamide oxygen/lysine3.28(192) interaction
Hurst, Dow,Umejiego, Uju,Lynch, Diane,Seltzman, Herbert,Hyatt, Steven,Roche, Michael,McAllister, Sean,Fleischer, Daniel,Kapur, Ankur,Abood, Mary,Shi, Shanping,Jones, Jannie,Lewis, Deborah,Reggio, Patricia
, p. 5969 - 5987 (2007/10/03)
The biarylpyrazole, N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4- dichlorophenyl)-4-methyl-1#-pyrazole-3-carboxamide (SR141716; 1) has been shown to act as an inverse agonist/antagonist at the cannabinoid CB1 receptor. Our previous mutant cycle study sugg
