122374-26-9Relevant articles and documents
Reductive Radical Conjugate Addition of Alkyl Electrophiles Catalyzed by a Cobalt/Iridium Photoredox System
Escobar, Randolph A.,Johannes, Jeffrey W.
supporting information, p. 6046 - 6051 (2021/08/03)
Alkyl and aryl halides have been studied extensively as radical precursors; however, mild and less toxic conditions for the activation of alkyl bromides toward alkyl radicals are still desirable. Reported here is a reductive radical conjugate addition tha
Design, synthesis and evaluation of new GEQ derivatives as inhibitors of InhA enzyme and Mycobacterium tuberculosis growth
Chollet, Aurélien,Mori, Giorgia,Menendez, Christophe,Rodriguez, Frédéric,Fabing, Isabelle,Pasca, Maria Rosalia,Madacki, Jan,Korduláková, Jana,Constant, Patricia,Quémard, Anna?k,Bernardes-Génisson, Vania,Lherbet, Christian,Baltas, Michel
supporting information, p. 218 - 235 (2015/07/07)
A series of fluorene-based derivatives was synthesized and evaluated for inhibiting both InhA and Mycobacterium tuberculosis growth. These compounds were inspired by the previously reported Genz-10850 molecule, a good InhA inhibitor, but with a poor activity against M. tuberculosis growth. Structure-activity relationships were performed by introducing the following chemical modifications: 1) the piperazine ring; 2) the amide group; 3) the aryl moiety; and 4) the fluorene moiety. Among these new derivatives, one of them was more effective against both the InhA activity and mycobacterial growth, compared to the hit compound. Docking studies were also performed to rationalize activities of these derivatives. Furthermore, we showed for the first time that efflux pump inhibitors potentiated the efficacy of Genz-10850 (GEQ) derivatives against M. tuberculosis growth, demonstrating that these compounds could be substrates of some efflux pumps.
Nickel-Catalyzed reductive cross-Coupling of unactivated alkyl halides
Yu, Xiaolong,Yang, Tao,Wang, Shulin,Xu, Hailiang,Gong, Hegui
, p. 2138 - 2141 (2011/06/22)
A Ni-catalyzed reductive approach to the cross-coupling of two unactivated alkyl halides has been successfully developed. The reaction works efficiently for primary and secondary halides, with at least one being bromide. The mild reaction conditions allow for excellent functional group tolerance and provide the C(sp3)-C(sp3) coupling products in moderate to excellent yields.