Synthesis of novel ligustrazine derivatives as NA+/H+ exchange inhibitors |
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| Authors: | Ren Mei Dong Jin Xu Yungen Wen Nan Gong Guoqing |
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| Institution: | 1. Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, P.?R. China, (phone: +86‐25‐8332?2067;2. fax: +86‐25‐8327?1487);3. Department of Pharmacology, China Pharmaceutical University, Nanjing 210009, P.?R. China, (phone: +86‐25‐8360?4316;4. fax: +86‐25‐8330?1606) |
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| Abstract: | 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 (IC50=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. |
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| Keywords: | Guanidine derivatives benzoyl‐ Ligustrazine derivatives Inhibitors Na+/H+ Exchange (NHE) inhibitors |
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