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二氢烷氧基苄基-氧代嘧啶衍生物(DABO)作为非核苷逆转录酶抑制剂:更新综述(2001-2011)。

Dihydro-alkoxyl-benzyl-oxopyrimidine derivatives (DABOs) as non-nucleoside reverse transcriptase inhibitors: an update review (2001-2011).

机构信息

Department of Chemistry, Fudan University, Shanghai 200433, People's Republic of China.

出版信息

Curr Med Chem. 2012;19(2):152-62. doi: 10.2174/092986712803414169.

Abstract

Numerous structurally different non-nucleoside compounds have been evaluated for their inhibitory effects against HIV replication, in which DABO derivatives, bearing the dihydro-alkoxyl-benzyl-oxopyrimidine scaffold, have been identified as a particular class of non-nucleoside reverse transcriptase inhibitors (NNRTIs). The S-DABO, NH-DABO, -N-DABO, DATNO and DACO analogs represent various structural chemical modifications of the substituents on C2, C6 and C5 of the pyrimidine ring to obtain potentially higher potency and lower cytotoxicity. This review article describes the recent progress of the chemical modifications and structure-activity relationship studies of DABO derivatives and provides new clues for the design of new DABO congeners.

摘要

已经评估了许多结构不同的非核苷化合物对 HIV 复制的抑制作用,其中含有二氢烷氧基苄基-氧嘧啶骨架的 DABO 衍生物被鉴定为一类特殊的非核苷逆转录酶抑制剂(NNRTIs)。S-DABO、NH-DABO、-N-DABO、DATNO 和 DACO 类似物代表了嘧啶环上 C2、C6 和 C5 取代基的各种结构化学修饰,以获得潜在更高的效力和更低的细胞毒性。本文综述了 DABO 衍生物的化学修饰和构效关系研究的最新进展,为新型 DABO 同系物的设计提供了新的线索。

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