Biomedical subjects
Publications and source records attributed to Kohtaro Goto.
Amino disaccharides having an alpha-(1-->4) linkage or a beta-(1-->4) linkage have been prepared as the mimics of amino glycoside antibiotics and their inhibition for HIV-1 TAR-Tat were examined. The compound having alpha-(1-->4) linkage denotes better inhibition for TAR-Tat than that of the one having beta-(1-->4).
The Bfp-OH, a novel fluorous protecting reagent, was able to be easily prepared. The Bfp group was readily introduced to a carbohydrate, removed in high yield, and recyclable after cleavage. The use of the Bfp group made it possible to synthesize a pentasaccharide by minimal column chromatography purification. Each synthetic intermediate was able to be easily purified only by simple fluorous-organic solvent extraction and monitored by TLC, NMR, and MS.
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Three new fluorous supports for peptide synthesis, i.e., the trialkoxybenzhydryl-type (6), the Wang-type (7) and the tert-butyl-type support (8), were prepared. A bioactive peptide TRH was easily synthesized by an Fmoc strategy using the benzhydryl-type fluorous support with fluorous chemistry.