- Palladium-catalyzed C-H bond carboxylation of acetanilides: An efficient usage of N,N-dimethyloxamic acid as the carboxylate source
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N,N-Dimethyloxamic acid can be successfully employed as a carboxylate precursor in the palladium-catalyzed direct C-H carboxylation of acetanilides. The reaction proceeds smoothly under mild conditions over a broad range of substrates with high functional group tolerance, affording substituted N-acyl anthranilic acids in moderate to high yields.
- Wu, Yinuo,Jiang, Cheng,Wu, Deyan,Gu, Qiong,Luo, Zhang-Yi,Luo, Hai-Bin
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supporting information
p. 1286 - 1289
(2016/01/15)
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- Synthesis and evaluation of quinazolines as inhibitors of the bacterial cell division protein FtsZ
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The bacterial cell division protein FtsZ is one of many potential targets for the development of novel antibiotics. Recently, zantrin Z3 was shown to be a cross-species inhibitor of FtsZ; however, its specific interactions with the protein are still unknown. Herein we report the synthesis of analogues that contain a more tractable core structure and an analogue with single-digit micromolar inhibition of FtsZs GTPase activity, which represents the most potent inhibitor of Escherichia coli FtsZ reported to date. In addition, the zantrin Z3 core has been converted to two potential photo-cross-linking reagents for proteomic studies that could shed light on the molecular interactions between FtsZ and molecules related to zantrin Z3.
- Nepomuceno, Gabriella M.,Chan, Katie M.,Huynh, Valerie,Martin, Kevin S.,Moore, Jared T.,Obrien, Terrence E.,Pollo, Luiz A. E.,Sarabia, Francisco J.,Tadeus, Clarissa,Yao, Zi,Anderson, David E.,Ames, James B.,Shaw, Jared T.
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supporting information
p. 308 - 312
(2015/03/30)
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- Anthranilic acid derivatives
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Agents for lowering glucose levels in blood having the formula: STR1 wherein Ro is bromo, chloro, fluoro, nitro or trifluoromethyl, R is hydrogen, C1-6 alkyl or C2-18 alkanoyl, and R1 is hydrogen or C1-12 alkyl, and the non-toxic, pharmaceutically acceptable salts thereof.
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