C2-symmetrical tetrahydroxyazepanes as inhibitors of glycosidases and HIV/FIV proteases.
Publication
, Journal Article
Qian, X; Morís-Varas, F; Fitzgerald, MC; Wong, CH
Published in: Bioorganic & medicinal chemistry
December 1996
C2-Symmetrical tetrahydroxyazepanes were synthesized as inhibitors for glycosidases. Tetrahydroxyazepane 1 is a non-specific inhibitor of various glycosidases, while compounds 2, 3 and 4 specifically inhibit beta-N-acetylglucosaminidase, beta-glucosidase, and alpha-fucosidase, respectively, with Ki in the micromolar range. Compound 1 is not an inhibitor of HIV/FIV proteases, but its 3,6-difluorobenzyl derivatives are moderate inhibitors of both enzymes.
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Published In
Bioorganic & medicinal chemistry
DOI
EISSN
1464-3391
ISSN
0968-0896
Publication Date
December 1996
Volume
4
Issue
12
Start / End Page
2055 / 2069
Related Subject Headings
- Structure-Activity Relationship
- Piperidines
- Models, Molecular
- Medicinal & Biomolecular Chemistry
- Imino Pyranoses
- HIV Protease Inhibitors
- Glycoside Hydrolases
- Enzyme Inhibitors
- Crystallography, X-Ray
- Azepines
Citation
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ICMJE
MLA
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Qian, X., Morís-Varas, F., Fitzgerald, M. C., & Wong, C. H. (1996). C2-symmetrical tetrahydroxyazepanes as inhibitors of glycosidases and HIV/FIV proteases. Bioorganic & Medicinal Chemistry, 4(12), 2055–2069. https://doi.org/10.1016/s0968-0896(96)00218-0
Qian, X., F. Morís-Varas, M. C. Fitzgerald, and C. H. Wong. “C2-symmetrical tetrahydroxyazepanes as inhibitors of glycosidases and HIV/FIV proteases.” Bioorganic & Medicinal Chemistry 4, no. 12 (December 1996): 2055–69. https://doi.org/10.1016/s0968-0896(96)00218-0.
Qian X, Morís-Varas F, Fitzgerald MC, Wong CH. C2-symmetrical tetrahydroxyazepanes as inhibitors of glycosidases and HIV/FIV proteases. Bioorganic & medicinal chemistry. 1996 Dec;4(12):2055–69.
Qian, X., et al. “C2-symmetrical tetrahydroxyazepanes as inhibitors of glycosidases and HIV/FIV proteases.” Bioorganic & Medicinal Chemistry, vol. 4, no. 12, Dec. 1996, pp. 2055–69. Epmc, doi:10.1016/s0968-0896(96)00218-0.
Qian X, Morís-Varas F, Fitzgerald MC, Wong CH. C2-symmetrical tetrahydroxyazepanes as inhibitors of glycosidases and HIV/FIV proteases. Bioorganic & medicinal chemistry. 1996 Dec;4(12):2055–2069.
Published In
Bioorganic & medicinal chemistry
DOI
EISSN
1464-3391
ISSN
0968-0896
Publication Date
December 1996
Volume
4
Issue
12
Start / End Page
2055 / 2069
Related Subject Headings
- Structure-Activity Relationship
- Piperidines
- Models, Molecular
- Medicinal & Biomolecular Chemistry
- Imino Pyranoses
- HIV Protease Inhibitors
- Glycoside Hydrolases
- Enzyme Inhibitors
- Crystallography, X-Ray
- Azepines