Design and synthesis of dual inhibitors of HIV reverse transcriptase and integrase: introducing a diketoacid functionality into delavirdine.

Wang Z; Vince R

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Design and synthesis of dual inhibitors of HIV reverse transcriptase and integrase: introducing a diketoacid functionality into delavirdine.

机译：Design and synthesis of dual inhibitors of HIV reverse transcriptase and integrase: introducing a diketoacid functionality into delavirdine.

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摘要

Cost and toxicity problems associated with highly active antiretroviral therapy (HAART) in HIV/AIDS treatment could be alleviated by using designed multiple ligands (DMLs). Dual inhibitors of HIV reverse transcriptase (RT) and integrase (IN) were rationally designed by introducing a diketoacid (DKA) functionality into the tolerant C-5 site of RT inhibitor delavirdine. The resulting compounds all demonstrate good activity against both RT and IN in enzymatic assays and HIV in cell-based assay, whereas their C-7 regioisomers are all inactive in these assays. Balanced activities were observed with C-3 halogenated inhibitors.

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《Bioorganic and medicinal chemistry》 |2008年第7期|3587-3595|共9页
作者
Wang Z; Vince R;
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作者单位

Center for Drug Design, Academic Health Center, University of Minnesota, 516 Delaware Street SE, Minneapolis, MN 55455, USA. wangx472@umn.edu;

ost.saga-med.ac.jp;

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原文格式 PDF
正文语种英语
中图分类药学;生物化学;
关键词
Delavirdine; Drug Design; HIV; HIV Integrase; HIV Integrase Inhibitors; HIV Reverse Transcriptase; 地拉韦定; 药物设计; HIV整合酶; HIV整合酶抑制剂; 酮酸类; 分子结构; 逆转录酶抑制剂;

Design and synthesis of dual inhibitors of HIV reverse transcriptase and integrase: introducing a diketoacid functionality into delavirdine.

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