17872-58-1Relevant 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
supporting information; experimental part, 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.
Dye derived from a pyrazolotriazole
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, (2008/06/13)
A method of retouching a dye image comprises selective removal with an aqueous acidic organic solvent solution, as described in the application, of a portion of a dye image from an exposed and processed photographic silver halide element comprising a support bearing a dye image from a dye-forming coupler and a primary amine photographic color developing agent, wherein the dye-forming coupler: (a) contains so ionizable group that is retained as part of a dye formed upon oxidative coupling, (b) has a structure such that the Log P of the coupler is greater than 4 and is derived from a four-equivalent coupler that has a Log P less than 8, and (c) has a coupling reactivity that enables formation of maximum image density of at least 0.6. The method comprises the step of contacting the dye image with an aqueous acidic organic solvent solution, as described in the application, for a time and at a temperature sufficient to selectively dissolve and remove a portion of the dye image from the photographic element. A new photographic element designed for such retouching comprises new pyrazolotriazole couplers as described in the application.