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

Novel N‐(2,2′‐disubstituted‐2H‐cromenyl)‐N′N″‐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 <...

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Veröffentlicht in:Bulletin of the Korean Chemical Society 2015, 36(9), , pp.2224-2229
Hauptverfasser: Lee, Gee-Hyung, Nam, Yeonju, Kim, Eun-Mi, Lim, Su-Jeong, Yang, Seung-Ju, Park, Kyuhee, Choi, Yongmun, Gong, Young-Dae
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Sprache:eng
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Zusammenfassung:Novel N‐(2,2′‐disubstituted‐2H‐cromenyl)‐N′N″‐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 μM). 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.
ISSN:1229-5949
0253-2964
1229-5949
DOI:10.1002/bkcs.10429