613656-45-4Relevant academic research and scientific papers
Oxygen-containing benzo-cycloaliphatic amine compounds
-
, (2018/06/16)
The invention provides an oxygen-containing benzo-cycloaliphatic substituted amine compounds and application thereof and specifically relates to the oxygen-containing benzo-cycloaliphatic substitutedamine compounds as shown in a formula I which is described in the specification or pharmaceutically acceptable salts thereof and application of the same to preparation of Staphylococcus aureus goldenpigment synthesis inhibitor type antibacterial agents.
Novel Staphyloxanthin Inhibitors with Improved Potency against Multidrug Resistant Staphylococcus aureus
Ni, Shuaishuai,Li, Baoli,Chen, Feifei,Wei, Hanwen,Mao, Fei,Liu, Yifu,Xu, Yixiang,Qiu, Xiaoxi,Li, Xiaokang,Liu, Wenwen,Hu, Linghao,Ling, Dazheng,Wang, Manjiong,Zheng, Xinyu,Zhu, Jin,Lan, Lefu,Li, Jian
, p. 233 - 237 (2018/03/21)
Diapophytoene desaturase (CrtN) is a potential novel target for intervening in the biosynthesis of the virulence factor staphyloxanthin. In this study, 38 1,4-benzodioxan-derived CrtN inhibitors were designed and synthesized to overwhelm the defects of leading compound 4a. Derivative 47 displayed superior pigment inhibitory activity, better hERG inhibitory properties and water solubility, and significantly sensitized MRSA strains to immune clearance in vitro. Notably, 47 displayed excellent efficacy against pigmented S. aureus Newman, Mu50 (vancomycin-intermediate MRSA, VISA), and NRS271 (linezolid-resistant MRSA, LRSA) comparable to that of linezolid and vancomycin in vivo.
Isoquinolines as IGF-1R Inhibitors
-
Page/Page column 11, (2009/04/24)
Compounds of the formula (I): were synthesized. In at least one embodiment, they were found to down-regulate or inhibit the expression or function of the IGF-1 receptor.
ISOQUINOLINES AS IGF-1R INHIBITORS
-
Page/Page column 38, (2010/11/26)
Compounds of the formula (I) were synthesized. They were found to down- regulate or inhibit the expression or function of the IGF-I receptor.
HETEROCYCLIC COMPOUNDS, METHODS OF MAKING THEM AND THEIR USE IN THERAPY
-
Page 88, (2010/02/07)
In part, the present invention is directed to antibacterial compounds of formula (I) wherein A is a bicyclic heteroaryl ring or a tricyclic ring and R2 is an heterocyclic residue; L is a bond, or L is alkyl, alkenyl or cycloalkyl.
