747383-57-9Relevant academic research and scientific papers
Design, synthesis, and structure–activity relationship study of potent mapk11 inhibitors
Gong, Mengdie,Li, Honglin,Li, Lu,Li, Shiliang,Sun, Hongxia,Tu, Mingyan,Zhao, Zhenjiang,Zhu, Lili
, (2022/01/04)
Huntington’s disease (HD) is a rare single-gene neurodegenerative disease, which can only be treated symptomatically. Currently, there are no approved drugs for HD on the market. Studies have found that MAPK11 can serve as a potential therapeutic target f
Crystallographic and SAR analyses reveal the high requirements needed to selectively and potently inhibit SIRT2 deacetylase and decanoylase
Yang, Ling-Ling,Xu, Wei,Yan, Jie,Su, Hui-Lin,Yuan, Chen,Li, Chao,Zhang, Xing,Yu, Zhu-Jun,Yan, Yu-Hang,Yu, Yamei,Chen, Qiang,Wang, Zhouyu,Li, Lin,Qian, Shan,Li, Guo-Bo
supporting information, p. 164 - 168 (2019/01/30)
A high-quality X-ray crystal structure reveals the mechanism of compound 1a inhibiting SIRT2 deacetylase and decanoylase. Structure-activity relationship (SAR) analysis of the synthesized derivatives of 1a reveals the high requirements needed for selectiv
Metal-Free Iodine-Catalyzed Direct Arylthiation of Substituted Anilines with Thiols
Yang, Daoshan,Yan, Kelu,Wei, Wei,Zhao, Jing,Zhang, Mengqi,Sheng, Xuguang,Li, Guoqing,Lu, Shenglei,Wang, Hua
, p. 6083 - 6092 (2015/06/30)
Iodine-catalyzed direct arylthiation of substituted anilines for the synthesis of various diaryl sulfides has been developed under metal- and solvent-free conditions. The present method uses readily available thiols as the arylthiation reagents, and envir
A very active Cu-catalytic system for the synthesis of aryl, heteroaryl, and vinyl sulfides
Kabir, M. Shahjahan,Lorenz, Michael,Van Linn, Michael L.,Namjoshi, Ojas A.,Ara, Shamim,Cook, James M.
experimental part, p. 3626 - 3643 (2010/07/14)
Figure presented cis-1,2-Cyclohexanediol (L3) has been shown to be an efficient and versatile bidentate O-donor ligand that provides a highly active Cu-catalytic system. It was more effective than diols such as trans-1,2-cyclohexanediol or ethylene glycol. This commercially available cis-1,2-cyclohexanediol ligand facilitated the Cu-catalyzed cross-coupling reactions of alkyl, aryl, or heterocyclic thiols with either alkyl, aryl, heterocyclic, or substituted vinyl halides. This new catalytic system promoted the mild and efficient stereo- and regiospecific synthesis of biologically important vinyl sulfides. The yields obtained using electron-rich substituted vinyl sulfides with this catalyst system are generally 75-98%. Most importantly, this singular catalyst system is extremely versatile and provides entry into a wide range of sulfides. This method is particularly noteworthy given its mild reaction conditions, simplicity, generality, and exceptional level of functional group tolerance.
Discovery and SAR development of 2-(phenylamino) imidazolines as postacyclin receptor antagonists
Clark, Robin D.,Jahangir, Alam,Severance, Daniel,Salazar, Rick,Chang, Thomas,Chang, David,Jett, Mary Frances,Smith, Steven,Bley, Keith
, p. 1053 - 1056 (2007/10/03)
On the basis of screening hits (1a,b), a series of selective, high affinity prostacyclin receptor antagonists was developed. The optimized lead compound 25d [(4,5-dihydro-1H-imidazol-2-yl)-[4-(4-isopropoxybenzyl)phenyl] amine] had analgesic activity in the rat.
4-Substituted anilides as selective melatonin MT2 receptor agonists
Epperson, James R.,Deskus, Jeffrey A.,Gentile, Anthony J.,Iben, Lawrence G.,Ryan, Elaine,Sarbin, Nathan S.
, p. 1023 - 1026 (2007/10/03)
A series of 4-substituted anilides with human melatonergic affinity is reported. Butyramides 26, 39, 42, 52, 57, and 58 all demonstrated subnanomolar MT2 binding affinity and MT2 selectivity of at least 70-fold over the MT1 receptor. Compound 26 demonstrated full agonism at the MT2 receptor.
