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Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors.

Bioorganic & medicinal chemistry (2012-05-18)
Xuwang Chen, Peng Zhan, Xin Liu, Ziheng Cheng, Caicai Meng, Siyuan Shao, Christophe Pannecouque, Erik De Clercq, Xinyong Liu
ABSTRACT

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 EC(50) values in low nanomolar concentration range (especially compound 6b3, EC(50) = 4.61 nM, SI = 5945) and high activity against K103N/Y181C resistant mutant strain of HIV-1 with EC(50) values in low micromolar concentration range. In addition, preliminary structure-activity relationship and molecular modeling of these new analogs were detailed in this manuscript.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Piperidine, ReagentPlus®, 99%
Sigma-Aldrich
Piperidine, ≥99.5%, purified by redistillation
Sigma-Aldrich
Piperidine solution, suitable for peptide synthesis, 20% in DMF
Sigma-Aldrich
Piperidine, biotech. grade, ≥99.5%
Sigma-Aldrich
Piperidine, puriss. p.a., ≥99.0% (GC/T)

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