A　series　of　N-aryl-2-arylthioacetamide　derivatives　(2-4)　designed　as　non-nucleoside　reverse　transcriptase　inhibitors　was　synthesized　and　evaluated　for　their　inhibitory　activity　against　HIV-1　(IIIB)　replication　in　MT-4　cell　cultures.　The　compounds　2-4　were　performed　by　the　reaction　of　thiols　and　2-chloro-N-substituted-acetamides　and　active　in　the　lower　micromolar　concentration　(1.25-20.83　mu　m).　The　studies　of　structure-activity　relationship　suggested　that　1H-benzo[d]imidazole　ring　at　arylthio　moiety　strongly　improved　the　anti-HIV　activity　and　consistent　with　the　experimental　data.　The　results　of　molecular　modeling　and　docking　within　the　RT　non-nucleoside　binding　site　using　AutoDock　confirmed　that　the　3　series,　similar　to　other　non-nucleoside　reverse　transcriptase　inhibitors　such　as　N-(5-chloro-2-pyridinyl)-N＇-[2-(4-ethoxy-3-fluoro-2-pyridinyl)ethyl]-thiourea　(PETT),　was　assumed　in　a　butterfly-like　conformation　and　helped　to　rationalize　some　SARs　and　the　biological　activity　data.