Design and synthesis of á, á-trehalose derivatives bearing guanidino groups as inhibitors for the Tat Protein-TAR RNA interaction of HIV-1 |
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基金项目: | Supported by the National Natural Science Foundation of China and Ph.D Program Fund of China. |
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摘 要: | Replication of human immunodeficiency virus type 1 (HIV-1) requires specific interactions of Tat protein with the transactivation responsive region (TAR) RNA. Disruption of Tat-TAR RNA interaction could inhibit HIV-1 replication. Here four target compounds were designed and synthesized to bind to TAR RNA for blocking the interaction of Tat-TAR RNA. The core molecule 6,6'-diamino-6,6' -dideoxy-α,α-trehalose was obtained from selective bromination of α,α-trehalose at C-6,6', fo…
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Design and synthesis of á,á-trehalose derivatives bearing guanidino groups as inhibitors for the Tat Protein-TAR RNA interaction of HIV-1 |
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Authors: | Wang Min XU Zhidong Tu Pengfei Xiao Sulong Yu Xiaolin Yang Ming |
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Abstract: | Replication of human immunodeficiency virus type 1 (HIV-1) requires specific interactions of Tat protein with the transactivation responsive region (TAR) RNA. Disruption of Tat-TAR RNA interaction could inhibit HIV-1 replication. Here four target compounds were designed and synthesized to bind to TAR RNA for blocking the interaction of Tat-TAR RNA. The core molecule 6,6′-diamino-6,6′ -dideoxy-á,á-trehalose was obtained from selective bromination of a,a-trehalose at C-6,6′, followed by acetylation, azide displacement, deacetylation and reduction.Coupling of the core molecule with the protected amino acid, then deprotection and guanidinylation generated 6,6′-bis(L-arginylamino)-6,6′-dideoxy-á,á-trehalose,6,6′-bisguanidino-6,6′-dideoxy-á ,á-trehalose, 6,6′-bis ((a)-guanidinobutyryl)amino]-6,6′-dideoxy-á,á-trehalose and 6,6′-bis(guanidinoacetylamino)-6,6′-dideoxy-á,á-trehalose, respectively.Their abilities to inhibit Tat-TAR RNA interaction were determined by a Tat-dependent HIV-1LTR-driven CAT assays. |
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Keywords: | á á-Trehalose derivative Guanidine group HIV-1 Tat-TAR interaction |
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