New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors
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- 作者：Valeria Famiglinia ; Giuseppe La Reginaa ; giuseppe.laregina@uniroma1.it" class="auth_mail ; Antonio Colucciaa ; Sveva Pellicciaa ; Andrea Brancaleb ; Giovanni Magac ; Emmanuele Crespanc ; Roger Badiad ; Bonaventura Clotetd ; José ; A. Esté ; d ; Roberto Cirillie ; Ettore Novellinof ; Romano Silvestria ; romano.silvestri@icloud.com" class="auth_mail
- 关键词：AIDS ; HIV-1 ; Reverse transcriptase ; Nonnucleoside inhibitor ; Indolylarylsulfone
- 刊名：European Journal of Medicinal Chemistry
- 出版年：10 June 2014
- 年：2014
- 卷：80
- 期：Complete
- 页码：101-111
- 全文大小：1256 K
文摘
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New indolylarylsulfones were prepared and evaluated as HIV-1 NNRTIs.
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Against the NL4-3 HIV-1 WT strain, compounds 4–15 were superior to reference drugs NVP and EFV.
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Several compounds inhibited the K103N HIV-1 mutant strain in the nanomolar range of concentration and were superior to EFV.
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Against the Y181C and L100I HIV-1 mutant strains, some compounds were superior to EFV.
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Enantiomer 24 was more potent than 25 against the whole viral panel.