Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1364752 | Bioorganic & Medicinal Chemistry Letters | 2008 | 4 Pages |
Abstract
Novel series of 3-amino-N-(4-aryl-1,1-dioxothian-4-yl)butanamides and 3-amino-N-(4-aryltetrahydropyran-4-yl)butanamides were synthesized and evaluated as dipeptidyl peptidase IV (DPP-IV) inhibitors. Derivatives incorporating the 6-substituted benzothiazole group showed highly potent DPP-IV inhibitory activity. Oral administration of (3R)-3-amino-4-(2,4,5-trifluorophenyl)-N-{4-[6-(2-methoxyethoxy)benzothiazol-2-yl]tetrahydropyran-4-yl}butanamide (12u) reduced blood glucose excursion in an oral glucose tolerance test.
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Related Topics
Physical Sciences and Engineering
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Organic Chemistry
Authors
Aiko Nitta, Hideaki Fujii, Satoshi Sakami, Yutaka Nishimura, Tomofumi Ohyama, Mikiya Satoh, Junko Nakaki, Shiho Satoh, Chifumi Inada, Hideki Kozono, Hiroki Kumagai, Masahiro Shimamura, Tominaga Fukazawa, Hideki Kawai,