104920-79-8Relevant academic research and scientific papers
Study on the synthesis and biological activities of α-substituted arylacetates derivatives
Liu, Jinbing,Chen, Changhong,Wu, Fengyan,Tang, Junyuan
, p. 1715 - 1719 (2016)
Anisodamine was isolated from the medicinal herb, it was used in the treatment of gastrointestinal smooth muscle spasm, infective toxic shock and organophosphorus intoxication. But there is no report about anisodamine with α-glucosidase inhibitory activity. In order to find novel α-glucosidase inhibitors, a series of α-substituted arylacetates derivatives have been synthesized based on the active unit of anisodamine. In α-glucosidase assay, compound 9 in Schiff base form and compound 22 in ester form show strong inhibition against α-glucosidase with IC50value of 46.81?μM and 83.76?μM, respectively. Compounds 9 and 22 exhibit comparable good antidiabetic activities as commercial drug Glimepiride. In addition, Schiff bases of α-substituted arylacetates show antitumor activities against human cancer cell lines, where compound 9 with thiourea moiety performs the best antitumor activity. We anticipate that our research will provide potential candidate scaffolds for antidiabetic drug design.
Synthesis and anticancer evaluation of 3-substituted quinolin-4-ones and 2,3-dihydroquinolin-4-ones
Rajput, Santosh,Gardner, Christopher R.,Failes, Timothy W.,Arndt, Greg M.,Black, David Stc.,Kumar, Naresh
, p. 105 - 115 (2014/01/17)
A series of 3-aryl-5,7-dimethoxyquinolin-4-ones 8 and 3-aryl-5,7-dimethoxy- 2,3-dihydroquinolin-4-ones 13 were synthesized in good yields. Demethylation under a range of conditions afforded the corresponding 5-hydroxy and 5,7-dihydroxy derivatives. Biolog
Lewis base catalyzed asymmetric hydrosilylation of α-substituted β-enamino esters: Facile access to enantioenriched β2-amino esters via dynamic kinetic resolution
Shu, Chang,Hu, Xiao-Yan,Li, Shuai-Shuai,Yuan, Wei-Cheng,Zhang, Xiao-Mei
supporting information, p. 1879 - 1882 (2014/08/18)
A chiral Lewis base organocatalyzed asymmetric hydrosilylation of α-substituted β-enamino esters is presented. The reactions proceeded through dynamic kinetic resolution to afford various enantioenriched β2-amino esters with high yields (up to
Discovery of isoxazolinone antibacterial agents. Nitrogen as a replacement for the stereogenic center found in oxazolidinone antibacterials
Snyder, Lawrence B.,Meng, Zhaoxing,Mate, Robert,D'Andrea, Stanley V.,Marinier, Anne,Quesnelle, Claude A.,Gill, Patrice,Den Bleyker, Kenneth L.,Fung-Tomc, Joan C.,Frosco, MaryBeth,Martel, Alain,Barrett, John F.,Bronson, Joanne J.
, p. 4735 - 4739 (2007/10/03)
A series of potential antimicrobial derivatives possessing bioisosteric replacements for the central oxazolidinone ring found in oxazolidinone antibacterials have been prepared. The design concept involved replacement of the requisite sp3-hybridized stereogenic center found at the 5-position of the oxazolidinone with a nitrogen atom. The synthesis and antibacterial activity of three such ring systems, the benzisoxazolinones, pyrroles, and isoxazolinones is described.
