18472-06-5Relevant articles and documents
Method of preparing Quinoline-5,8-dione derivatives for TGase 2 inhibitor
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, (2020/04/28)
I Is -5,8- of the quinoline, dione derivative compound. of Formula I, or a stereoisomer or a pharmaceutically acceptable salt thereof, wherein the compound of Formula, TGase 2 has, inhibitory effects TGase 2, and thus the pharmaceutical composition may be useful for preventing or treating disorders or diseases mediated by TGase 2 or inhibiting. (by machine translation)
Direct ortho-Selective Amination of 2-Naphthol and Its Analogues with Hydrazines
Jia, Lei,Tang, Qiang,Luo, Meiming,Zeng, Xiaoming
, p. 5082 - 5091 (2018/05/15)
Described herein is a regioselective ortho-amination of 2-naphthol and its analogues with substituted hydrazines. It provides a direct methodology for the synthesis of N-arylaminated naphthol derivatives without the formation of related 1,1′-biaryl-2,2′-diamine or carbazole byproducts. Specifically, using N,N-disubstituted hydrazine precursors, N-unsubstituted ortho-aminated derivatives and related secondary amines can be formed in ethylene glycol in moderate to excellent yields. Variation of substrates to N,N′-diarylhydrazines and N-methyl-N,N′-diarylhydrazines led to N-aryl-1-amino-2-naphthol compounds. It is noted that biologically interesting indazole motifs can be facilely created by the reaction of N,N′-dialkylhydrazines with 2-naphthols. These ortho-amination reactions have the advantage of one-pot operation without the use of transition metal catalysts.
Identifying chelators for metalloprotein inhibitors using a fragment-based approach
Jacobsen, Jennifer A.,Fullagar, Jessica L.,Miller, Melissa T.,Cohen, Seth M.
experimental part, p. 591 - 602 (2011/03/21)
Fragment-based lead design (FBLD) has been used to identify new metal-binding groups for metalloenzyme inhibitors. When screened at 1 mM, a chelator fragment library (CFL-1.1) of 96 compounds produced hit rates ranging from 29% to 43% for five matrix meta
