52727-62-5Relevant articles and documents
Optimization of a binding fragment targeting the “enlarged methionine pocket” leads to potent Trypanosoma brucei methionyl-tRNA synthetase inhibitors
Huang, Wenlin,Zhang, Zhongsheng,Ranade, Ranae M.,Gillespie, J. Robert,Barros-álvarez, Ximena,Creason, Sharon A.,Shibata, Sayaka,Verlinde, Christophe L.M.J.,Hol, Wim G.J.,Buckner, Frederick S.,Fan, Erkang
supporting information, p. 2702 - 2707 (2017/05/29)
Potent inhibitors of Trypanosoma brucei methionyl-tRNA synthetase were previously designed using a structure-guided approach. Compounds 1 and 2 were the most active compounds in the cyclic and linear linker series, respectively. To further improve cellular potency, SAR investigation of a binding fragment targeting the “enlarged methionine pocket” (EMP) was performed. The optimization led to the identification of a 6,8-dichloro-tetrahydroquinoline ring as a favorable fragment to bind the EMP. Replacement of 3,5-dichloro-benzyl group (the EMP binding fragment) of inhibitor 2 using this tetrahydroquinoline fragment resulted in compound 13, that exhibited an EC50 of 4?nM.
Synthesis of 2,6-disubstituted and 2,3,6-trisubstituted anilines
Pews,Hunter,Wehrmeyer
, p. 4809 - 4820 (2007/10/02)
A number of 2,6-disubstituted and 2,3,6-trisubstituted anilines have been prepared via the selective para dehalogenation of the corresponding anilines. Modification of the substituents on the amino nitrogen demonstrates that the selectivity is derived from steric rather than electronic effects. The effects of the choice of formate hydrogen donor, Pd catalyst, solvent, and temperature upon the efficiency and selectivity of the dehalogenation are discussed.
Oxidation von Isatinen zu Anthranilsaeureestern
Reissenweber, Gernot,Mangold, Dietrich
, p. 914 - 915 (2007/10/02)
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