期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 16, 期 8, 页码 2105-2108出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.01.073
关键词
AIDS; HIV; reverse transcriptase; inhibitor; oxindole; SAR
A novel oxindole was discovered as an HIV non-nucleoside reverse transcriptase inhibitor via HTS using a cell-based assay. Systematic structural modifications were carried out to establish its SAR. These modifications led to the identification of oxindoles with low nanomolar potency for inhibiting HIV replication. These novel and potent oxindoles could serve as advanced leads for further optimizations. (C) 2006 Elsevier Ltd. All rights reserved.
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