Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 20, Issue 12, Pages 3856-3864Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2012.04.030
Keywords
HIV-1; NNRTIs; Piperidine; Triazine; Antiviral activity; SAR; Molecular modeling
Funding
- National Natural Science Foundation of China (NSFC) [81102320, 30873133, 30772629, 30371686]
- NSFC [30910103908]
- Research Fund for the Doctoral Program of Higher Education of China [20110131130005, 20110131120037]
- Independent Innovation Foundation of Shandong University (IIFSDU) [2010GN044]
- Shandong Postdoctoral Innovation Science Research Special Program [201002023]
- China Postdoctoral Science Foundation [20100481282]
- KU Leuven [GOA 10/014]
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A novel series of piperidine-linked amino-triazine derivatives were designed, synthesized and evaluated for in vitro anti-HIV activity as non-nucleoside reverse transcriptase inhibitors on the basis of our previous work. Screening results indicated that most compounds showed excellent activity against wild-type HIV-1 with EC50 values in low nanomolar concentration range (especially compound 6b3, EC50 = 4.61 nM, SI = 5945) and high activity against K103N/Y181C resistant mutant strain of HIV-1 with EC50 values in low micromolar concentration range. In addition, preliminary structure-activity relationship and molecular modeling of these new analogs were detailed in this manuscript. Crown Copyright (C) 2012 Published by Elsevier Ltd. All rights reserved.
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