- Palladium catalyzed domino C-H activation strategy: An access to 9- fluorenones
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Palladium catalyzed domino C-H functionalization reaction of arylaldehyde with dihaloarene has been developed to access 9-flourenone molecules. Bidentate ligand assisted strategy, single step reaction, high yield and excellent functional group tolerance make this method concise and effective for the synthesis of 9-flourenone. In addition, proposed method has been successfully employed to synthesise Tilorone in gram scale.
- Patel, Anuj,Shaikh, Mahommedumar,Chikhalia, Kishor
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supporting information
p. 236 - 245
(2018/12/11)
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- Design, synthesis and evaluation of new GEQ derivatives as inhibitors of InhA enzyme and Mycobacterium tuberculosis growth
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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.
- 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
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p. 218 - 235
(2015/07/07)
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- Synthesis of fluorenone derivatives through Pd-catalyzed dehydrogenative cyclization
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Palladium-catalyzed dual C-H functionalization of benzophenones to form fluorenones by oxidative dehydrogenative cyclization is reported. This method provides a concise and effective route toward the synthesis of fluorenone derivatives, which shows outstanding functional group compatibility.
- Li, Hu,Zhu, Ru-Yi,Shi, Wen-Juan,He, Ke-Han,Shi, Zhang-Jie
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supporting information
p. 4850 - 4853,4
(2012/12/12)
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- Bisphenolic compounds that enhance cell cation transport are found in commercial phenol red
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We have isolated two bisphenolic compounds (4 and 5) that have a marked effect on K+ and Na+ concentrations in human cells from commercial preparations of the pH indicator dye phenol red (phenolsulfonphthalein). We used a bioassay to
- Kym, Philip R.,Hummert, Kim L.,Nilsson, Anna G.,Lubin, Martin,Katzenellenbogen, John A.
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p. 4897 - 4904
(2007/10/03)
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