Novel analogs of N -acylhydroxyethylaminomethyl-4 H -chromen-4-one scaffold as IL-5 inhibitors

Hyun-Sun Yang; Eeda Venkateswararao; Pulla Reddy BogguVinay K. SharmaYoungsoo KimSang-Hun Jung

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Novel analogs of N -acylhydroxyethylaminomethyl-4 H -chromen-4-one scaffold as IL-5 inhibitors

机译：Novel analogs of N -acylhydroxyethylaminomethyl-4 H -chromen-4-one scaffold as IL-5 inhibitors

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Graphical abstract Display Omitted Abstract A number of N -acyl substituted hydroxyethylaminomethyl-4 H -chromen-4-ones 6a – u were prepared and evaluated for their IL-5 inhibitory activity. Among them, the compound 6r (95.0% inhibition at 30 μM, IC 50 = 10.0 μM, C log P = 4.1549) showed most potent inhibitory activity. The structure activity relationship revealed that the bulkier or hydrophobic substituents at urea, carbamate or amide group resulted in good inhibitory activity against IL-5. Moreover, electron donating group at phenyl ring ( 6g and 6s ) is much more active than electron withdrawing group ( 6f ). Finally, replacement of cyclohexylmethoxy group at 5 th position of ring A with bulky aliphatic substituents resulted in the loss of activity. ]]>

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来源
《Bioorganic and medicinal chemistry》 |2017年第16期|4330-4338|共9页
作者
Hyun-Sun Yang; Eeda Venkateswararao; Pulla Reddy BogguVinay K. SharmaYoungsoo KimSang-Hun Jung;
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作者单位

College of Pharmacy and Institute of Drug Research and Development, Chungnam National University;

College of Pharmacy, Chungbuk National University;

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原文格式 PDF
正文语种英语
中图分类药学;
关键词
Chromen-4-one analogs; Inhibitor; Interleukin-5; Eosinophil; Asthma;

Novel analogs of N -acylhydroxyethylaminomethyl-4 H -chromen-4-one scaffold as IL-5 inhibitors

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