75782-99-9Relevant academic research and scientific papers
C-H activation guided by aromatic N-H ketimines: Synthesis of functionalized isoquinolines using benzyl azides and alkynes
Gupta, Sreya,Han, Junghoon,Kim, Yongjin,Lee, Soon W.,Rhee, Young Ho,Park, Jaiwook
, p. 9094 - 9103 (2014/12/11)
Aromatic N-H ketimines were in situ generated from various benzylic azides by ruthenium catalysis for the subsequent Rh-catalyzed annulation reaction with alkynes to give the corresponding isoquinolines. In contrast to conventional synthetic methods for aromatic N-H ketimines, our protocol works under mild and neutral conditions, which enabled the synthesis of isoquinolines having various functionalities such as carbonyl, ester, alkenyl, and ether groups. In addition, the imidates generated from α-azido ethers were successfully used for the synthesis of 1-alkoxyisoquinolines.
Design, synthesis, and biological evaluation of novel 2-pyridinyl-[1,2,4] triazoles as inhibitors of transforming growth factor β1 type 1 receptor
Kim, Dae-Kee,Kim, Joonseop,Park, Hyun-Ju
, p. 2013 - 2020 (2007/10/03)
A series of 2-pyridinyl-[1,2,4]triazoles have been synthesized and evaluated for their ALK5 inhibitory activity in the luciferase reporter assays. Compound 12b showed significant ALK5 inhibition (SBE-Luciferase, 73%; p3TP-Luciferase, 85%) at a concentration of 5μM that is comparable to that of SB-431542 (SBE-Luciferase, 79%; p3TP-Luciferase, 88%), but weak p38α MAP kinase inhibition (4%) at a concentration of 10μM that is much lower than that of SB-431542 (54%). The binding mode of 12b generated by flexible docking studies revealed that the structure of 12b is a good fit into the (NPC-30345)-binding cavity of ALK5.
Carboximidamide derivatives
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, (2008/06/13)
Novel carboximidamide derivatives represented by the following formula (A) and acid adduct salts thereof are disclosed: STR1 wherein all the substituents have the same meanings as defined above. N-cyano-pyridinecarboximidate compounds represented by the f
