Citation: Wang Yujie, Upul Halambage, Zeng Chengchu, Hu Liming. Design, Synthesis, and Biological Activity of Novel Octahydro-1Hpyrrolo[3, 2-c]pyridine Derivatives as C-C Chemokine Receptor Type 5 (CCR5) Antagonists[J]. Chinese Journal of Organic Chemistry, ;2017, 37(9): 2385-2391. doi: 10.6023/cjoc201701049 shu

Design, Synthesis, and Biological Activity of Novel Octahydro-1Hpyrrolo[3, 2-c]pyridine Derivatives as C-C Chemokine Receptor Type 5 (CCR5) Antagonists

a.
College of Life Science and Bioengineering, Beijing University of Technology, Beijing 100124
b.
Beijing Key Laboratory of Environmental and Viral Oncology, Beijing University of Technology, Beijing 100124
c.
Department of Pathology, Microbiology and Immunology, Vanderbilt University Medical Center, Nashville 27232

Corresponding author: Hu Liming, huliming@bjut.edu.cn
Received Date: 13 February 2017
Revised Date: 3 April 2017
Available Online: 2 September 2017

Figures(4)

A series of novel octahydro-1H-pyrrolo[3, 2-c]pyridine derivatives were designed and synthesized as C-C chemokine receptor type 5 (CCR5) antagonists, and their biological activity of anti-human immunodeficiency virus type 1 (HIV-1) is evaluated. A majority of these compounds showed anti-HIV-1 activities. Octahydro-1H-pyrrolo[3, 2-c]pyridine derivative 19c exhibited potency against HIV-1 replication less than 1 μmol·L^-1. Function assay was employed and the result showed that there were other drug targets for HIV-1 inhibition besides CCR5. In addition, the preliminary structure-activity relationship (SAR) of these compounds was rationalized by docking studies.
- HIV-1,
- CCR5 antagonists,
- piperidine derivatives,
- structure-activity relationships
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