1248544-12-8Relevant articles and documents
Design and synthesis of several small-size HTLV-I protease inhibitors with different hydrophilicity profiles
Nguyen, Jeffrey-Tri,Kato, Keiko,Hidaka, Koushi,Kumada, Henri-Obadja,Kimura, Tooru,Kiso, Yoshiaki
, p. 2425 - 2429 (2011/06/17)
The human T cell leukemia/lymphotropic virus type 1 (HTLV-I) is clinically associated with adult T cell leukemia/lymphoma, HTLV-I associated myelopathy/tropical spastic paraparesis, and a number of other chronic inflammatory diseases. To stop the replication of the virus, we developed highly potent tetrapeptidic HTLV-I protease inhibitors. In a recent X-ray crystallography study, several of our inhibitors could not form co-crystal complexes with the protease due to their high hydrophobicity. In the current study, we designed, synthesized and evaluated the HTLV-I protease inhibition potency of compounds with hydrophilic end-capping moieties with the aim of improving pharmaceutic and pharmacokinetic properties.