6297-10-5Relevant articles and documents
A novel series of 4-methyl substituted pyrazole derivatives as potent glucagon receptor antagonists: Design, synthesis and evaluation of biological activities
Shu, Shuangjie,Dai, Antao,Wang, Jiang,Wang, Bin,Feng, Yang,Li, Jia,Cai, Xiaoqing,Yang, Dehua,Ma, Dakota,Wang, Ming-Wei,Liu, Hong
, p. 1896 - 1908 (2018/03/12)
A novel series of 4-methyl substituted pyrazole derivatives were designed, synthesized and biologically evaluated as potent glucagon receptor (GCGR) antagonists. In this study, compounds 9q, 9r, 19d and 19e showed high GCGR binding (IC50 = 0.09 μM, 0.06 μM, 0.07 μM and 0.08 μM, respectively) and cyclic-adenosine monophosphate (cAMP) activities (IC50 = 0.22 μM, 0.26 μM, 0.44 μM and 0.46 μM, respectively) in cell-based assays. Most importantly, the docking experiment demonstrated that compound 9r formed extensive hydrophobic interactions with the receptor binding pocket, making it justifiable to further investigate the potential of becoming a GCGR antagonist.
Direct conversion of aromatic ketones to arenecarboxylic esters via carbon-carbon bond-cleavage reactions
Yin, Guodong,Gao, Meng,Wang, Zihua,Wu, Yandong,Wu, Anxin
experimental part, p. 369 - 372 (2009/04/07)
Aromatic methyl ketones, ss-keto esters, and trifluoromethyl-l,3- diketones can be directly converted to arene-carboxylic esters via carbon-carbon bond cleavage of pyridinium iodide intermediates in the presence of copper(II) oxide, iodine, pyridine, and potassium carbonate in alcoholic media. The advantages of the present method in terms of good yields, mild reaction conditions, and inexpensive reagents should make this protocol a valuable alternative to the existing methods.
Synthesis and biological activities of 3-aminomethyl-1,2-dihydronaphthalene derivatives
Itoh,Miyake,Tanabe,Hirata,Oka
, p. 2006 - 2015 (2007/10/02)
A series of 3-aminomethyl-1,2-dihydronaphthalene derivatives was prepared from the corresponding 3,4-dihydro-1(2H)-naphthalenone derivatives in three steps, namely the Mannich reaction, reduction of the carbonyl group with sodium borohydride, and dehydrat
