43101-10-6Relevant academic research and scientific papers
MALT1 MODULATORS AND USES THEREOF
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Paragraph 00120; 00178, (2021/07/10)
Provided herein are compounds, compositions, and methods useful for modulating MALT1 and for treating related diseases, disorders, and conditions.
Design, synthesis and biological evaluation of novel 2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole triazole derivatives as potent TRPV1 antagonists
Li, Jinyu,Nie, Cunbin,Qiao, Yue,Hu, Jing,Li, Qifei,Wang, Qiang,Pu, Xiaohui,Yan, Lin,Qian, Hai
, p. 433 - 445 (2019/06/18)
Reported herein is the design, synthesis, and pharmacologic evaluation of a class of TRPV1 antagonists constructed on 2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole as A-region and triazole as B-region. The SAR analysis indicated that 2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole analogues displayed excellent antagonism of hTRPV1 activation by capsaicin and showed better potency compared to the corresponding dihydroindole analogues. Optimization of this design led to the eventual identification of 2-((1-(2-(trifluoromethyl)phenyl)-1H-1,2,3-triazol-4-yl)methyl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole (6g), a potent TRPV1 antagonist. In vitro, using cells expressing recombinant human TRPV1 channels, 6g displayed potent antagonism activated by capsaicin (IC50 = 0.075 μM) and only partially blocked acid activation of TRPV1. In vivo, 6g exhibited good efficacy in capsaicin-induced and heat-induced pain models and had almost no hyperthermia side-effect. Furthermore, pharmacokinetic studies revealed that compound 6g had a superior oral exposure after oral administration in rats. To understand its binding interactions with the receptor, the docking study of 6g was performed in rTRPV1 model and showed an excellent fit to the binding site. On the basis of its superior profiles, 6g could be considered as the lead candidate for the further development of antinociceptive drugs.
Synthesis, pharmacological evaluation and molecular modeling studies of triazole containing dopamine D3 receptor ligands
Peng, Xin,Wang, Qi,Mishra, Yogesh,Xu, Jinbin,Reichert, David E.,Malik, Maninder,Taylor, Michelle,Luedtke, Robert R.,Mach, Robert H.
supporting information, p. 519 - 523 (2015/03/05)
A series of 2-methoxyphenyl piperazine analogues containing a triazole ring were synthesized and their in vitro binding affinities at human dopamine D2 and D3 receptors were evaluated. Compounds 5b, 5c, 5d, and 4g, demonstrate high a
Photolysis of Quinolyl and Isoquinolyl Azides in Primary and Secondary Aliphatic Amines: Synthesis of Bicyclic Azepines, Diazepines, and Quinolyl- and Isoquinolyl-diamines
Hollywood, Frank,Nay, Barry,Scriven, Eric F. V.,Suschitzky, Hans,Khan, Zafar U.,Hull, Roy
, p. 421 - 429 (2007/10/02)
Photolysis of the title compounds in primary aliphatic amines gave in some cases bicyclic azepines and diazepines as well as o-diamines, while in secondary amines mainly the appropriate o-diamines are obtained.On the basis of the many examples studied guidelines are put forward to predict the nature of products from photolysis of bicyclic azides in primary and secondary amines and to obtain maximum yields.
