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2006 Indole derivatives R 0140 Design, Synthesis and Biological Evaluations of Novel Oxindoles as HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors. Part 1. — Compound (VIa) shows the highest antiviral effects of all products tested. Derivative (VIb) exhibits high antiviral activity whereas the bulkier analogue (VIc) is completely inactive. These re- sults show that the cyclopropane region is sensitive to small perturbation. — (JIANG, T.; KUHEN, K. L.; WOLFF, K.; YIN, H.; BIEZA, K.; CALDWELL, J.; BURSULAYA, B.; WU, T. Y.-H.; HE*, Y.; Bioorg. Med. Chem. Lett. 16 (2006) 8, 2105-2108; Genomics Inst., Novartis Res. Found., San Diego, CA 92121, USA; Eng.) — C. Oppel 29- 096

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Page 1: Design, Synthesis and Biological Evaluations of Novel Oxindoles as HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors. Part 1

2006

Indole derivativesR 0140 Design, Synthesis and Biological Evaluations of Novel Oxindoles as HIV-1

Non-Nucleoside Reverse Transcriptase Inhibitors. Part 1. — Compound (VIa) shows the highest antiviral effects of all products tested. Derivative (VIb) exhibits high antiviral activity whereas the bulkier analogue (VIc) is completely inactive. These re-sults show that the cyclopropane region is sensitive to small perturbation. — (JIANG, T.; KUHEN, K. L.; WOLFF, K.; YIN, H.; BIEZA, K.; CALDWELL, J.; BURSULAYA, B.; WU, T. Y.-H.; HE*, Y.; Bioorg. Med. Chem. Lett. 16 (2006) 8, 2105-2108; Genomics Inst., Novartis Res. Found., San Diego, CA 92121, USA; Eng.) — C. Oppel

29- 096

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