6297-10-5Relevant academic research and scientific papers
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.
Trisubstituted imidazoles as mycobacterium tuberculosis glutamine synthetase inhibitors
Gising, Johan,Nilsson, Mikael T.,Odell, Luke R.,Yahiaoui, Samir,Lindh, Martin,Iyer, Harini,Sinha, Achyut M.,Srinivasa, Bachally R.,Larhed, Mats,Mowbray, Sherry L.,Karlén, Anders
supporting information; experimental part, p. 2894 - 2898 (2012/06/01)
Mycobacterium tuberculosis glutamine synthetase (MtGS) is a promising target for antituberculosis drug discovery. In a recent high-throughput screening study we identified several classes of MtGS inhibitors targeting the ATP-binding site. We now explore o
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.
Solvolyses of naphthoyl chlorides. Solvent effect and Grunwald-Winstein correlation analyses with YxBnCl scales
Liu, Kwang-Ting,Hwang, Patty Y.-H.,Chen, Hun-I.
, p. 750 - 757 (2007/10/03)
The solvolyses of 1-naphthoyl (2), 2-naphthoyl (3), 4-methyl-1-naphthoyl (4) and 6-methoxy-2-naphthoyl (5) chlorides in a variety of solvents were studied, and correlation analyses by using the single- and dual-parameter Grunwald-Winstein equations were examined. An excellent linear relationship (R = 0.995) for 4, log (k/k0) = 0.733YxBnCl + 0.269NOTs, was observed. An SN1-like mechanism with decreasing extent of nucleophilic solvent participation was found in the solvolysis of 2 and 4.2-Naphthoyl chloride is likely to have a mechanism at the borderline of SN1-like dissociation and an addition-elimination process. 6-Methoxy-2-naphthoyl chloride shows more SN1-like character than 3 and is associated with nucleophilic solvent intervention more pronounced than that for 2 and 4. The applicability and the advantages of using the YxBnCl scale for different types of substrates are discussed. Copyright
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
