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초록
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.
키워드
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
- 제목
- Novel N-(2,2 '-disubstituted-2H-cromenyl)-N ',N ''-disubstituted Guanidine Derivatives as an S-Nitrosoglutathion Reductase Inhibitor
- 저자
- Lee, Gee-Hyung; Nam, Yeonju; Kim, Eun-Mi; Lim, Su-Jeong; Yang, Seung-Ju; Park, Kyuhee; Choi, Yongmun; Gong, Young-Dae
- 발행일
- 2015-09
- 유형
- Article
- 권
- 36
- 호
- 9
- 페이지
- 2224 ~ 2229