Novel N-(2,2′-disubstituted-2H-cromenyl)-N′,N"-disubstituted Guanidine Derivatives as an S-Nitrosoglutathion Reductase Inhibitor

被引:1
|
作者
Lee, Gee-Hyung [1 ]
Nam, Yeonju [2 ]
Kim, Eun-Mi [1 ]
Lim, Su-Jeong [1 ]
Yang, Seung-Ju [1 ]
Park, Kyuhee [2 ]
Choi, Yongmun [2 ]
Gong, Young-Dae [1 ]
机构
[1] Dongguk Univ, Coll Sci, Innovat Drug Lib Res Ctr, Dept Chem, Seoul 100715, South Korea
[2] Gyeonggi Inst Sci & Technol Promot, Gyeonggi Bio Ctr, Suwon 443270, South Korea
关键词
Anti-inflammatory inhibitor; S-Nitrosoglutathion reductase; Drug-like library; Guanidine derivatives; SOLID-PHASE SYNTHESIS; DEPENDENT FORMALDEHYDE DEHYDROGENASE; EXPERIMENTAL ASTHMA; PARALLEL SYNTHESIS; LINKER; BRONCHODILATOR; NITROSYLATION; LIBRARY;
D O I
10.1002/bkcs.10429
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Novel N-(2,20-disubstituted-2H-cromenyl)-N0N00-disubstituted guanidine derivatives were synthesized and evaluated as an S-nitrosoglutathion (GSNO) reductase inhibitor. The synthesized guanidine derivatives 1 and 2b showed high potency in an enzyme-based assay with recombinant GSNO reductase (IC50 < 10 mu M). Surface plasmon resonance measurement and molecular docking studies confirmed the direct interaction of compound 2b with GSNO reductase. The results provide valuable information for the design of inhibitors with better spectrum of activity toward GSNO reductase.
引用
收藏
页码:2224 / 2229
页数:6
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