718632-63-4Relevant academic research and scientific papers
Design, Synthesis, and Evaluation of Reversible and Irreversible Monoacylglycerol Lipase Positron Emission Tomography (PET) Tracers Using a "tail Switching" Strategy on a Piperazinyl Azetidine Skeleton
Chen, Zhen,Mori, Wakana,Deng, Xiaoyun,Cheng, Ran,Ogasawara, Daisuke,Zhang, Genwei,Schafroth, Michael A.,Dahl, Kenneth,Fu, Hualong,Hatori, Akiko,Shao, Tuo,Zhang, Yiding,Yamasaki, Tomoteru,Zhang, Xiaofei,Rong, Jian,Yu, Qingzhen,Hu, Kuan,Fujinaga, Masayuki,Xie, Lin,Kumata, Katsushi,Gou, Yuancheng,Chen, Jingjin,Gu, Shuyin,Bao, Liang,Wang, Lu,Collier, Thomas Lee,Vasdev, Neil,Shao, Yihan,Ma, Jun-An,Cravatt, Benjamin F.,Fowler, Christopher,Josephson, Lee,Zhang, Ming-Rong,Liang, Steven H.
supporting information, p. 3336 - 3353 (2019/03/29)
Monoacylglycerol lipase (MAGL) is a serine hydrolase that degrades 2-arachidonoylglycerol (2-AG) in the endocannabinoid system (eCB). Selective inhibition of MAGL has emerged as a potential therapeutic approach for the treatment of diverse pathological co
Rational Design, Synthesis, and Biological Evaluation of Heterocyclic Quinolones Targeting the Respiratory Chain of Mycobacterium tuberculosis
Hong, W. David,Gibbons, Peter D.,Leung, Suet C.,Amewu, Richard,Stocks, Paul A.,Stachulski, Andrew,Horta, Pedro,Cristiano, Maria L. S.,Shone, Alison E.,Moss, Darren,Ardrey, Alison,Sharma, Raman,Warman, Ashley J.,Bedingfield, Paul T. P.,Fisher, Nicholas E.,Aljayyoussi, Ghaith,Mead, Sally,Caws, Maxine,Berry, Neil G.,Ward, Stephen A.,Biagini, Giancarlo A.,O’Neill, Paul M.,Nixon, Gemma L.
supporting information, p. 3703 - 3726 (2017/05/19)
A high-throughput screen (HTS) was undertaken against the respiratory chain dehydrogenase component, NADH:menaquinone oxidoreductase (Ndh) of Mycobacterium tuberculosis (Mtb). The 11000 compounds were selected for the HTS based on the known phenothiazine Ndh inhibitors, trifluoperazine and thioridazine. Combined HTS (11000 compounds) and in-house screening of a limited number of quinolones (50 compounds) identified ～100 hits and four distinct chemotypes, the most promising of which contained the quinolone core. Subsequent Mtb screening of the complete in-house quinolone library (350 compounds) identified a further ～90 hits across three quinolone subtemplates. Quinolones containing the amine-based side chain were selected as the pharmacophore for further modification, resulting in metabolically stable quinolones effective against multi drug resistant (MDR) Mtb. The lead compound, 42a (MTC420), displays acceptable antituberculosis activity (Mtb IC50 = 525 nM, Mtb Wayne IC50 = 76 nM, and MDR Mtb patient isolates IC50 = 140 nM) and favorable pharmacokinetic and toxicological profiles.
SUBSTITUTED PYRROLO-PYRAZOLE DERIVATIVES AS KINASE INHIBITORS
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Page 58, (2008/06/13)
Compounds represented by formula (Ia) or (lb) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disor
