Discovery of potent, selective, bioavailable phosphodiesterase 2 (PDE2) inhibitors active in an osteoarthritis pain model, part I: transformation of selective pyrazolodiazepinone phosphodiesterase 4 (PDE4) inhibitors into selective PDE2 inhibitors.
作者:
主题词
动物(Animals);氮呤类(Azirines);结合部位(Binding Sites);催化域(Catalytic Domain);结晶学, X线(Crystallography, X-Ray);环核苷酸磷酸二酯酶类, 2型(Cyclic Nucleotide Phosphodiesterases, Type 2);环核苷酸磷酸二酯酶类, 4型(Cyclic Nucleotide Phosphodiesterases, Type 4);二氢吡啶类(Dihydropyridines);疾病模型, 动物(Disease Models, Animal);药物评价, 临床前(Drug Evaluation, Preclinical);骨关节炎(Osteoarthritis);磷酸二酯酶4抑制剂(Phosphodiesterase 4 Inhibitors);磷酸二酯酶抑制剂(Phosphodiesterase Inhibitors);蛋白质结合(Protein Binding);构效关系(Structure-Activity Relationship)
DOI
10.1016/j.bmcl.2013.03.072
PMID
23582272
发布时间
2013-05-10
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