674782-58-2Relevant articles and documents
RADIOLABELED SUGARS FOR IMAGING OF FUNGAL INFECTIONS
-
Page/Page column 28; 30, (2021/02/12)
Disclosed herein are compounds having a structure according to Formula I and optionally Formula IV. Formula I Formula IV. The compounds may be radiolabeled compounds useful for diagnosis and/or imaging fungal infections. In such embodiments, at least one substituent is a radionuclide, such as 18F. Also disclosed are precursor compounds according to Formula I and/or IV that are useful for making the radiolabeled compounds. In such embodiments, the precursor compound comprises at least one leaving group suitable for introducing a radionuclide, such as 18F, at a desired position. Also disclosed are methods for making and using the compounds, including embodiments of a method for imaging and/or diagnosing a fungal infection in a subject.
Radiosynthesis of 18F-labeled D-allose
Yamamoto, Hiroyuki,Wada, Kenji,Toyohara, Jun,Tago, Tetsuro,Ibaraki, Masanobu,Kinoshita, Toshibumi,Yamamoto, Yuka,Nishiyama, Yoshihiro,Kudomi, Nobuyuki
, (2019/10/05)
Rare sugars are defined as monosaccharides that exist in nature but are only present in limited quantities. D-Allose is a rare sugar that has been reported to have some unique physiological effects. The present study describes suitable synthetic procedures for novel rare sugars of D-allose that are 18F-labeled at the C-3 and C-6 positions and the preparation of the appropriate labeling precursors. The goal is to facilitate in vivo, noninvasive positron emission tomography (PET) investigation of the behavior of rare sugar analogs of D-allose in organs. We found five precursors that were practical for labeling, three for 3-deoxy-3-[18F]fluoro-D-allose ([18F]3FDA) and two for 6-deoxy-6-[18F]fluoro-D-allose ([18F]6FDA). With manual operation synthesis, the highest radiochemical conversion rates were 75% for [18F]3FDA with a precursor of 1,2,4,6-tetra-O-acetyl-3-O-trifluoromethanesulfonyl-β-D-glucopyranose and 69% for [18F]6FDA with a precursor of 1,2,3,4-tetra-O-acetyl-6-O-trifluoromethanesulfonyl-β-D-allopyranose. Furthermore, the practical yields of [18F]3FDA and [18F]6FDA using an automated synthesizer were also investigated. Radiochemical yields of 67% and 49% were obtained for [18F]3FDA and [18F]6FDA, respectively, in an automated synthesizer. As basic assessment of stability for use in PET scanning, high performance liquid chromatography analysis showed no decomposition of [18F]3FDA and [18F]6FDA after up to 6 h in rabbit blood plasma.
BIARYL AMIDES WITH MODIFIED SUGAR GROUPS FOR TREATMENT OF DISEASES ASSOCIATED WITH HEAT SHOCK PROTEIN PATHWAY
-
Page/Page column 165; 180; 224-225, (2019/12/04)
Provided are biaryl amides and coumarin-based compounds with modified sugar groups for treatment of diseases associated with heat shock protein pathway. The compounds having the following formulas, wherein variables are as defined herein. Formulae (I), (II), (III), (IV), and (V), Pharmaceutical compositions of the compounds are also provided. These biaryl amides and coumarin-based derivatives with modified sugar groups are useful for treatment and prevention of diseases and disorders, including neurological disorders, such as neurodegenerative diseases and nerve damaging disorders, for example, diabetic peripheral neuropathy.
