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[期刊论文]
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Structure-activity relationships of first bishydroxymethyl-substituted cage dimeric 4-aryl-1,4-dihydropyridines as HIV-1 protease inhibitors
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作 者：
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Andreas Hilgeroth;Hauke Lilie;
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出版年：2003
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页 码：495 - 499
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出版社：Elsevier BV
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摘 要：
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A first series of novel bishydroxymethyl-substituted cage dimeric 4-aryl-1,4-dihydropyridines 5-8 has been synthesised and evaluated as HIV-1 protease and HIV-inhibitors in vitro assays. Moderate activity data of protease inhibition have been found for of theN-Boc substituted compound 8. Reduced activity for compound 6 and almost no residual activity of 5 and 7 emphasise the importance of the tert. butyl substituent for protease inhibitory activity thus supporting a discussed probable binding of the N-acyloxy substituent to the S2/S2' regions of protease.
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关键字：
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Cage dimeric 4-aryl-1,4-dihydropyridines;HIV-1 protease inhibitor;Binding region
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所属期刊
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ISSN: 0223-5234
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来自：Elsevier BV
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