非钙依赖性磷酸二酯酶喹唑啉二酮抑制剂的构效关系
Structure-activity relationship of quinazolinedione inhibitors of calcium-independent phosphodiesterase.
作者信息
Lowe J A, Archer R L, Chapin D S, Chen J B, Helweg D, Johnson J L, Koe B K, Lebel L A, Moore P F, Nielsen J A
机构信息
Central Research Division Pfizer, Inc. Groton, Connecticut 06340.
出版信息
J Med Chem. 1991 Feb;34(2):624-8. doi: 10.1021/jm00106a024.
A series of quinazolinediones and azaquinazolinediones is described which possess potent inhibitory activity toward the calcium-independent phosphodiesterase enzyme (CaIPDE). In vivo testing showed that this in vitro activity translates to animal models predictive of chronic diseases such as depression and inflammation. These results support the hypothesis that inhibition of CaIPDE may lead to useful activity in such chronic diseases.
描述了一系列喹唑啉二酮和氮杂喹唑啉二酮，它们对钙非依赖性磷酸二酯酶（CaIPDE）具有强效抑制活性。体内试验表明，这种体外活性在预测抑郁症和炎症等慢性疾病的动物模型中得到体现。这些结果支持了以下假设：抑制CaIPDE可能会在这类慢性疾病中产生有益的活性。
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