105776-76-9Relevant academic research and scientific papers
Synthesis and antimicrobial activity of some isoindolin-1-ones derivatives
Breytenbach, Jaco C.,Van Dyk, Sandra,Van Den Heever, Ilse,Allin, Steven M.,Hodkinson, Claire C.,Northfield, Christopher J.,Page, Micheal I.
, p. 1629 - 1631 (2000)
A range of N-substituted isoindolin-1-ones was prepared and their potential as novel antimicrobial agents was investigated. MIC values for active compounds were determined and reported. (C) 2000 Published by Elsevier Science Ltd.
Erinacerins c-l, isoindolin-1-ones with α-glucosidase inhibitory activity from cultures of the medicinal mushroom hericium erinaceus
Wang, Kai,Bao, Li,Qi, Qiuyue,Zhao, Feng,Ma, Ke,Pei, Yunfei,Liu, Hongwei
, p. 146 - 154 (2015)
The well-known edible and medicinal mushroom Hericium erinaceus produces various bioactive secondary metabolites. Ten new isoindolin-1-ones, named erinacerins C-L (1-10), together with (E)-5-(3,7-dimethylocta-2,6-dien-1-yl)-4-hydroxy-6-methoxy-2-phenethylisoindolin-1-one (11) were isolated from the solid culture of H. erinaceus. The structures of new metabolites were established by spectroscopic methods. The absolute configurations of 3, 4, 9, and 10 were assigned by comparing their specific rotations with those of related phthalimidines (13-20). Compounds 5 and 6, 7 and 8, and 9 and 10 are double-bond positional isomers. In a α-glucosidase inhibition assay, compounds 2-11 showed inhibitory activity with IC50 values ranging from 5.3 to 145.1 μM. Preliminary structure-activity analysis indicated that the terpenoid side chain and the phenolic hydroxy groups contributed greatly to the α-glucosidase inhibitory activity of 1-11. In a cytotoxicity assay, compound 11 also presented weak cytotoxicity against two cell lines, A549 and HeLa, with IC50 values of 49.0 and 40.5 μM.
USP30 INHIBITORS AND USES THEREOF
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Paragraph 00749-00750, (2021/03/19)
The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of USP30, and the treatment of USP30-mediated disorders.
New Modified Heterocyclic Phenylalanine Derivatives. Incorporation into Potent Inhibitors of Human Renin
Ocain, Timothy D.,Deininger, David D.,Russo, Ralph,Senko, Nancie A.,Katz, Alan,et al.
, p. 823 - 832 (2007/10/02)
Modified heterocyclic phenylalanine analogues designed as replacements for the P3-P4 region were synthesized and incorporated into renin inhibitors.These inhibitors were found to have significant activity versus human recombinant renin, as well as in vivo activity.The compounds proved to be very resistant to chymotrypsin degradation, as exemplified by compound 8, which remained greater than 60percent intact after a 24-h exposure to chymotrypsin.In contrast, the Boc-Phe analogue was nearly completely degraded after 1 h.Compound 6 proved to be the most potent renin inhibitor with an IC50=8.9 nM.These stable cyclized phenylalanines should prove to be generally useful as a substitute for Boc-Phe in protease inhibitors.
