952433-45-3Relevant academic research and scientific papers
Copper-Catalyzed Intermolecular Enantioselective Radical Oxidative C(sp3)?H/C(sp)?H Cross-Coupling with Rationally Designed Oxazoline-Derived N,N,P(O)-Ligands
Gu, Qiang-Shuai,Guo, Kai-Xin,Li, Zhong-Liang,Liu, Lin,Liu, Xin-Yuan,Tian, Yu,Yang, Chang-Jiang,Ye, Liu
supporting information, p. 26710 - 26717 (2021/11/18)
The intermolecular asymmetric radical oxidative C(sp3)?C(sp) cross-coupling of C(sp3)?H bonds with readily available terminal alkynes is a promising method to forge chiral C(sp3)?C(sp) bonds because of the high atom and step economy, but remains underexplored. Here, we report a copper-catalyzed asymmetric C(sp3)?C(sp) cross-coupling of (hetero)benzylic and (cyclic)allylic C?H bonds with terminal alkynes that occurs with high to excellent enantioselectivity. Critical to the success is the rational design of chiral oxazoline-derived N,N,P(O)-ligands that not only tolerate the strong oxidative conditions which are requisite for intermolecular hydrogen atom abstraction (HAA) processes but also induce the challenging enantiocontrol. Direct access to a range of synthetically useful chiral benzylic alkynes and 1,4-enynes, high site-selectivity among similar C(sp3)?H bonds, and facile synthesis of enantioenriched medicinally relevant compounds make this approach very attractive.
From triclosan toward the clinic: Discovery of nonbiocidal, potent FabI inhibitors for the treatment of resistant bacteria
Gerusz, Vincent,Denis, Alexis,Faivre, Fabien,Bonvin, Yannick,Oxoby, Mayalen,Briet, Sophia,LeFralliec, Géraldine,Oliveira, Chrystelle,Desroy, Nicolas,Raymond, Cédric,Peltier, La?titia,Moreau, Fran?ois,Escaich, Sonia,Vongsouthi, Vanida,Floquet, Stéphanie,Drocourt, Elodie,Walton, Armelle,Prouvensier, Laure,Saccomani, Marc,Durant, Lionel,Genevard, Jean-Marie,Sam-Sambo, Vanessa,Soulama-Mouze, Coralie
supporting information, p. 9914 - 9928 (2013/01/16)
In this paper, we present some elements of our optimization program to decouple triclosan's specific FabI effect from its nonspecific cytotoxic component. The implementation of this strategy delivered highly specific, potent, and nonbiocidal new FabI inhibitors. We also disclose some preclinical data of one of their representatives, 83, a novel antibacterial compound active against resistant staphylococci and some clinically relevant Gram negative bacteria that is currently undergoing clinical trials.
Hydroxyphenyl derivatives and biological applications thereof
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Page/Page column 8-9, (2008/06/13)
The invention relates to hydroxyphenyl derivatives of formula (I) and the pharmaceutically acceptable salts, the organic and mineral salts, the racemic and each non racemic derivatives, the cis (Z) and Lrans (E) isomers the tautomers. Application particularly as anti-bacterial and/or anti-parasite agents.
