613-30-9Relevant articles and documents
Synthesis and biological evaluation of 2-quinolineacrylamides
Chen, Mei-Chuan,Chen, Shiou-Sheng,Hsu, Fu-Chun,Lee, Hsueh-Yun,Lin, Mei-Hsiang,Liou, Jing-Ping,Liu, Yi-Ting,Wang, Shih-Wei
, (2020)
A series of C6-substituted N-hydroxy-2-quinolineacrylamides (3–15), with four types of bridging groups have been synthesized. Most of these compounds exhibit antiproliferative activity against A549 and HCT116 cells and Western blot analysis revealed that they are able to inhibit HDAC. Measurement of the HDAC isoform activity of ether-containing compounds showed that compound 9 has distinct HDAC6 selectivity, more than 300-fold over other isoforms. This paper describes the development of 6-aryloxy-N-hydroxy-2-quinolineacrylamides as potential HDAC6 inhibitors.
Discovery and Biological Evaluation of a Novel Highly Potent Selective Butyrylcholinsterase Inhibitor
Li, Qi,Xing, Shuaishuai,Chen, Ying,Liao, Qinghong,Xiong, Baichen,He, Siyu,Lu, Weixuan,Liu, Yang,Yang, Hongyu,Li, Qihang,Feng, Feng,Liu, Wenyuan,Chen, Yao,Sun, Haopeng
, p. 10030 - 10044 (2020/10/18)
To discover novel BChE inhibitors, a hierarchical virtual screening protocol followed by biochemical evaluation was applied. The most potent compound 8012-9656 (eqBChE IC50 = 0.18 ± 0.03 μM, hBChE IC50 = 0.32 ± 0.07 μM) was purchased and synthesized. It inhibited BChE in a noncompetitive manner and could occupy the binding pocket forming diverse interactions with the target. 8012-9656 was proven to be safe in vivo and in vitro and showed comparable performance in ameliorating the scopolamine-induced cognition impairment to tacrine. Additionally, treatment with 8012-9656 could almost entirely recover the Aβ1-42 (icv)-impaired cognitive function to the normal level and showed better behavioral performance than donepezil. The evaluation of the Aβ1-42 total amount confirmed its anti-amyloidogenic profile. Moreover, 8012-9656 possessed blood-brain barrier (BBB) penetrating ability, a long T1/2, and low intrinsic clearance. Hence, the novel potential BChE inhibitor 8012-9656 can be considered as a promising lead compound for further investigation of anti-AD agents.
Continuous Flow Doebner-Miller Reaction and Isolation Using Continuous Stirred Tank Reactors
Yadav, Maruti B.,Kulkarni, Sourabh,Joshi, Ramesh A.,Kulkarni, Amol A.
supporting information, p. 1621 - 1625 (2016/09/23)
Continuous flow Doebner-Miller synthesis of different quinaldines from respective anilines is demonstrated using sulfuric acid as a homogeneous catalyst. The extent of reaction was monitored for various parameters, namely, temperature, residence time, mole ratio of sulfuric acid to substrate, mole ratio of crotonaldehyde to substrate, and so forth. Continuous stirred reactors in series were used as a preferred configuration for this rection that generates byproduct in the form of sticky solid material. The approach has been extended for six different anilines, and the results are compared with batch reactions. Continuous stirred reactors in series with distributed dosing of crotonaldehyde facilitated a continuous flow reaction with lower byproduct formation, increased yields, and continuous workup and is a scalable approach.
