216 resultados para sostituzione aromatica, derivati amminotiazolici, sali di diazonio, 1,3,5-Trinitrobenzene, meccanismi di reazione


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In continuation of our program aimed at the discovery and development of compounds with superior anti-human immunodeficiency virus type 1 (HIV-1) activity, 21N-arylsulfonyl-3-acetylindole analogs (2a-u) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro. Among of all the analogs, several compounds exhibited significant anti-HIV-1 activity, especially N-phenylsulfonyl-3-acetyl-6-methylindole (2j) and N-(p-ethyl)phenylsulfonyl-3-acetyl-6-methylindole (2n) showed the most potent anti-HIV-1 activity with EC50 values of 0.36 and 0.13 mu g/mL, and TI values of >555.55 and 791.85, respectively. It demonstrated that introduction of the acetyl group at the 3-position of N-arylsulfonyl-6-methylindoles could generally lead to the more potent analogs. (C) 2010 Elsevier Ltd. All rights reserved.

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Submitted by zhangdi (zhangdi@red.semi.ac.cn) on 2009-04-13T11:45:31Z

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Submitted by zhangdi (zhangdi@red.semi.ac.cn) on 2009-04-13T11:45:31Z

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Submitted by zhangdi (zhangdi@red.semi.ac.cn) on 2009-04-13T11:45:31Z

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Submitted by zhangdi (zhangdi@red.semi.ac.cn) on 2009-04-13T11:45:31Z

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Submitted by zhangdi (zhangdi@red.semi.ac.cn) on 2009-04-13T11:45:31Z

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Submitted by zhangdi (zhangdi@red.semi.ac.cn) on 2009-04-13T11:45:31Z

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Submitted by zhangdi (zhangdi@red.semi.ac.cn) on 2009-04-13T11:45:31Z

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Submitted by zhangdi (zhangdi@red.semi.ac.cn) on 2009-06-04T08:36:34Z No. of bitstreams: 1 dspace.cfg: 33388 bytes, checksum: ac9630d3fdb36a155287a049e8b34eb7 (MD5)

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Submitted by zhangdi (zhangdi@red.semi.ac.cn) on 2009-06-04T08:36:34Z No. of bitstreams: 1 dspace.cfg: 33388 bytes, checksum: ac9630d3fdb36a155287a049e8b34eb7 (MD5)

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Submitted by zhangdi (zhangdi@red.semi.ac.cn) on 2009-06-04T08:36:34Z No. of bitstreams: 1 dspace.cfg: 33388 bytes, checksum: ac9630d3fdb36a155287a049e8b34eb7 (MD5)