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Bioorg Med Chem ; 26(12): 3158-3165, 2018 07 23.
Article in English | MEDLINE | ID: mdl-29699911

ABSTRACT

A series of new 6-styryl-naphthalene-2-amidrazone derivatives were synthesized and evaluated as potential ASIC1a inhibitors. Among them, compound 5e showed the most activity to inhibit [Ca2+]i. elevation in acid-induced articular chondrocytes. Together with the important role of ASIC1a in the pathogenesis of tissue acidification diseases including rheumatoid arthritis, these results might provide a meaningful hint or inspiration in developing drugs targeting at tissue acidification diseases.


Subject(s)
Carboxylic Acids/chemistry , Drug Design , Sodium Channel Agonists/chemical synthesis , Acid Sensing Ion Channels/chemistry , Acid Sensing Ion Channels/metabolism , Animals , Calcium/metabolism , Carboxylic Acids/chemical synthesis , Carboxylic Acids/pharmacology , Cell Survival/drug effects , Cells, Cultured , Chondrocytes/cytology , Chondrocytes/metabolism , Naphthalenes/chemistry , Rats , Sodium Channel Agonists/chemistry , Sodium Channel Agonists/pharmacology , Structure-Activity Relationship
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