473258-22-9Relevant academic research and scientific papers
Simple, short peptide derivatives of a sulfonylindolecarboxamide (L-737,126) active in vitro against HIV-1 wild type and variants carrying non-nucleoside reverse transcriptase inhibitor resistance mutations
Silvestri, Romano,Artico, Marino,De Martino, Gabriella,La Regina, Giuseppe,Loddo, Roberta,La Colla, Massimiliano,La Colla, Paolo
, p. 3892 - 3896 (2004)
Non-nucleoside reverse transcriptase inhibitors (NNRTIs) active against NNRTI-resistant mutants were obtained by introducing two methyl groups at positions 3 and 5 of the benzenesulfonyl moiety of L-737,126 (1) and coupling one to three glycinamide/alanin
Indolylarylsulfones bearing phenylboronic acid and phenylboronate ester functionalities as potent HIV?1 non-nucleoside reverse transcriptase inhibitors
Xu, Shujing,Song, Shu,Sun, Lin,Gao, Ping,Gao, Shenghua,Ma, Yue,Kang, Dongwei,Cheng, Yusen,Zhang, Xujie,Cherukupalli, Srinivasulu,De Clercq, Erik,Pannecouque, Christophe,Liu, Xinyong,Zhan, Peng
, (2021/12/10)
To explore the chemical space around the entrance channel of the HIV-1 reverse transcriptase (RT) binding pocket, we innovatively designed and synthesized a series of novel indolylarylsulfones (IASs) bearing phenylboronic acid and phenylboronate ester fun
Indole aryl sulfone derivative as well as preparation method and application thereof
-
, (2021/06/06)
The invention provides an indole aryl sulfone derivative as well as a preparation method and application thereof. The derivative has a structure as shown in a general formula I or II. The invention also relates to a preparation method of the derivative an
Indole aryl sulfone derivative containing boric acid as well as preparation method and application thereof
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, (2021/06/09)
The invention provides an indole aryl sulfone derivative containing boric acid. The indole aryl sulfone derivative has a structure as shown in general formulas I, II or III. The invention also relates to a preparation method of the derivative and applicat
Discovery of novel indolylarylsulfones as potent HIV-1 NNRTIs via structure-guided scaffold morphing
Zhao, Tong,Meng, Qing,Kang, Dongwei,Ji, Jianbo,De Clercq, Erik,Pannecouque, Christophe,Liu, Xinyong,Zhan, Peng
, (2019/08/20)
For more in-depth exploration of the chemical space around the entrance channel of HIV-1 reverse transcriptase (RT), a series of novel indolylarylsulfones (IASs) bearing different chiral N-substituted pyrrolidine, azetidine or substituted sulfonamide grou
Discovery of novel piperidine-substituted indolylarylsulfones as potent HIV NNRTIs via structure-guided scaffold morphing and fragment rearrangement
Li, Xiao,Gao, Ping,Huang, Boshi,Zhou, Zhongxia,Yu, Zhao,Yuan, Zheng,Liu, Huiqing,Pannecouque, Christophe,Daelemans, Dirk,De Clercq, Erik,Zhan, Peng,Liu, Xinyong
, p. 190 - 201 (2016/10/25)
To further explore the chemical space around the entrance channel of HIV-1 reverse transcriptase (RT), a series of novel indolylarylsulfones (IASs) bearing N-substituted piperidine at indole-2-carboxamide were identified as potent HIV NNRTIs by structure-
Indolylarylsulfones bearing natural and unnatural amino acids. discovery of potent inhibitors of hiv-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie b4 virus
Piscitelli, Francesco,Coluccia, Antonio,Brancale, Andrea,La Regina, Giuseppe,Sansone, Anna,Giordano, Cesare,Balzarini, Jan,Maga, Giovanni,Zanoli, Samantha,Samuele, Alberta,Cirilli, Roberto,La Torre, Francesco,Lavecchia, Antonio,Novellino, Ettore,Silvestri, Romano
experimental part, p. 1922 - 1934 (2009/12/31)
New potent indolylarylsulfone (IAS) HIV-1 NNRTIs were obtained by coupling natural and unnatural amino acids to the 2-carboxamide and introducing different electron-withdrawing substituents at position 4 and 5 of the indole nucleus. The new IASs inhibited
