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Synthesis of Novel Ligustrazine Derivatives as Na + /H + Exchange Inhibitors
Author(s) -
Ren Mei,
Dong Jin,
Xu Yungen,
Wen Nan,
Gong Guoqing
Publication year - 2010
Publication title -
chemistry and biodiversity
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.427
H-Index - 70
eISSN - 1612-1880
pISSN - 1612-1872
DOI - 10.1002/cbdv.200900353
Subject(s) - chemistry , in vivo , ring (chemistry) , guanidine , benzene , stereochemistry , medicinal chemistry , biochemistry , organic chemistry , microbiology and biotechnology , biology
A novel series of 3,5,6‐trimethylpyrazine‐2‐methoxy (or methylamino) substituted benzoyl‐guanidine derivatives were designed and synthesized as Na + /H + exchange (NHE) inhibitors. In this study, compounds with electron‐withdrawing substituents on the benzene ring seemed to improve NHE‐1 inhibitory activities. Compounds 6d, 6k , and 6l were found to be potent inhibitors of NHE‐1 ( IC 50 =3.0±1.6, 3.0±1.4, and 1.6±0.4 nmol/l, resp.). Furthermore, they showed a remarkable reduction of infarct size in the rat myocardial infarction model in vivo.