9-BENZYL-6-(DIMETHYLAMINO)-9H-PURINES WITH ANTIRHINOVIRUS ACTIVITY
9-BENZYL-6-(DIMETHYLAMINO)-9H-PURINES WITH ANTIRHINOVIRUS ACTIVITY
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DOI：
10.1021/jm00118a025
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发表时间：
1988-10-01
影响因子：
7.3
通讯作者：
SELWAY, JWT
中科院分区：
文献类型：
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作者：
KELLEY, JL;LINN, JA;SELWAY, JWT
合成了一系列9-苄基-6-（二甲氨基）- 9h -嘌呤和9-苄基-2-氯-6-（二甲氨基）- 9h -嘌呤，并在细胞培养中检测了它们对1B型鼻病毒的活性。2位未被取代的9-苄基嘌呤活性较弱。然而，引入2-氯取代基导致抗病毒活性大幅增加。其中活性最高的化合物2-氯-6-（二甲氨基）-9-（4-甲基苄基）- 9h -嘌呤（29）的IC50值为0.08 .mu。抗血清型1B。四种化合物对其他18种鼻病毒血清型进行了测试，但大多数测试的敏感性低于1B型。29例血清型敏感性范围为0.08 ~ 14.m。这些9-苄基-2-氯- 9h -嘌呤代表了一类具有体外抗鼻病毒活性的新型抗病毒药物。
A series of 9-benzyl-6-(dimethylamino)-9H-purines and 9-benzyl-2-chloro-6-(dimethylamino)-9H-purines were synthesized and tested in cell culture for activity against rhinovirus type 1B. The 9-benzylpurines that were unsubstituted in the 2-position had weak activity. However, introduction of a 2-chloro substituent resulted in a substantial increase in antiviral activity. One of the most active compounds, 2-chloro-6-(dimethylamino)-9-(4-methylbenzyl)-9H-purine (29), had an IC50 value of 0.08 .mu.M against serotype 1B. Four compounds were tested against 18 other rhinovirus serotypes, but the majority tested were less sensitive than type 1B. The range of serotype sensitivity for 29 varied from 0.08 to 14 .mu.M. These 9-benzyl-2-chloro-9H-purines represent a new class of antiviral agents with in vitro activity against rhinoviruses.