61657-65-6Relevant academic research and scientific papers
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.
NITROGENOUS CYCLIC KETONE DERIVATIVE, PROCESS FOR PRODUCING THE SAME, AND USE
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Page 71-72, (2010/02/08)
A novel compound represented by the formula (I): wherein rings A and B each represents an optionally substituted aromatic ring, or rings A and B may be bonded to each other through linking between bonds or substituents thereof to form a ring; ring C represents a nitrogenous saturated heterocycle optionally having one or more substituents besides the oxo (provided that 2,3-dioxopyrrolidine ring is excluded); R1 represents hydrogen, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group; and-------- indicates a single bond or a double bond. It has high antagonistic activity against a tachykinin receptor, especially an SP receptor.
3,5-Dibromo-2-methoxybenzoic acid from sea sponge Didiscus sp.
Utkina,Fedoreyev,Ilyin,Antipin
, p. 2292 - 2294 (2007/10/03)
3,5-Dibromo-2-methoxybenzoic acid was isolated from sea sponge Didiscus sp. The structure of the title compound was established by spectral methods, by X-ray diffraction analysis, and by comparing with a synthetic sample prepared from salicylaldehyde.
