66644-22-2Relevant academic research and scientific papers
Design, synthesis and evaluation of novel molecules with a diphenyl ether nucleus as potential antitubercular agents
Yang, Yinghong,Wang, Zhenling,Yang, Jianzhong,Yang, Tao,Pi, Weiyi,Ang, Wei,Lin, Yanni,Liu, Yuanyuan,Li, Zicheng,Luo, Youfu,Wei, Yuquan
supporting information; experimental part, p. 954 - 957 (2012/03/11)
A series of compounds with a diphenyl ether nucleus were synthesized by incorporating various amines into the diphenyl ether scaffold with an amide bond. Their antitubercular activities were evaluated against Mycobacterium tuberculosis H37Rv by a microdilution method, with MIC values ranging from 4 to 64 μg/mL. Through structure-activity relationship studies, the two chlorine atoms at 3 and 4 positions in the phenyl ring of R2 group were found to play a significant role in the antitubercular activity. The most potent compound 6c showed an MIC value of 4 μg/mL and a good safety profile in HepG2 cell line by the MTT assay. Compound 6c was further found to be effective in a murine model of BCG infection, providing a good lead for subsequent optimization.
Alkadiene derivatives, their preparation, and pharmaceutical compositions containing them
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, (2008/06/13)
Substituted alkadienes of the formula: STR1 in which R1 is hydroxy or acetoxy, R2 is hydrogen, carboxy, alkoxycarbonyl, phenyl or benzoyl, and R3 is alkylthio or alkoxy and R4 is naphthoyl or optionally substituted benzoyl, or R3 is alkoxycarbonyl, cycloalkyloxycarbonyl or cyano and R4 is alkyl, naphthyl, optionally substituted phenyl, alkylthio, naphthylmethanethio, optionally substituted benzylthio, optionally substituted phenylthio, naphthylthio, phenethylthio or allylthio, or R3 and R4 form, with the carbon atom to which they are attached, a ring-system of formula: STR2 in which R5 is hydrogen or alkoxy and X is methylene or S inhibit 5-lipoxygenase and are useful, for example, as anti-inflammatories.
