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　mu　mol　circle　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.