Anti-AIDS agents 90. novel C-28 modified bevirimat analogues as potent HIV maturation inhibitors

K Qian, ID Bori, CH Chen, L Huang…

文献索引：Qian, Keduo; Bori, Ibrahim D.; Chen, Chin-Ho; Huang, Li; Lee, Kuo-Hsiung Journal of Medicinal Chemistry, 2012 , vol. 55, # 18 p. 8128 - 8136

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被引用次数: 34

摘要

In a continuing study of bevirimat (2), the anti-HIV-maturation clinical trials agent, 28 new betulinic acid (BA, 1) derivatives were designed and synthesized. Among these compounds, 17, with a C-28 MEM ester moiety, and 22, with a C-28 ethyl hexanoate, increased the anti- HIV replication activity compared with 2 by 2-fold while compounds 40, 41, 48, and 49, with C-28 piperazine or piperidine amide substitutions, increased the activity by 3-to 15-fold. ...