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Strategy for ~14C-IabeIIng of a series of bis(heteroaryl)piperazines

机译:一系列双(杂芳基)哌嗪〜14C-IabeIIng的策略

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摘要

Bis(heteroaryl)piperazines (BHAPs) have been a rich source of biologically active molecular entities and are related to a wide family of compounds with well-known pharmacological properties. A variety of analogues of BHAPs (such as: U-80493E) were synthesized and evaluated for their inhibition of human immunodeficiency virus typei reverse transcriptase. Sometimes replacement of the substituted aryl moiety with various aromatic systems provided bis (heteroaryl) piperazines that were10-100 fold more potent than U-80493E (for instance: Atevirdine).
机译:双(杂芳基)哌嗪(BHAP)是生物活性分子实体的丰富来源,并且与具有众所周知药理学性质的多种化合物有关。合成了多种BHAP类似物(例如:U-80493E),并评估了它们对人免疫缺陷病毒Typei逆转录酶的抑制作用。有时,用各种芳族体系取代取代的芳基部分可提供比U-80493E(例如Atevirdine)强10-100倍的双(杂芳基)哌嗪。

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