Design and synthesis of 3-pyridylacetamide derivatives as dipeptidyl peptidase IV (DPP-4) inhibitors targeting a bidentate interaction with Arg125

Synthesis and biological evaluation of our dipeptidyl peptidase IV (DPP-4) inhibitor were performed, and compound 13j with the potent activity were identified. We have previously discovered nicotinic acid derivative 1 as a structurally novel dipeptidyl peptidase IV (DPP-4) inhibitor. In this study,...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2011-01, Vol.19 (1), p.172-185
Hauptverfasser:	Miyamoto, Yasufumi, Banno, Yoshihiro, Yamashita, Tohru, Fujimoto, Tatsuhiko, Oi, Satoru, Moritoh, Yusuke, Asakawa, Tomoko, Kataoka, Osamu, Takeuchi, Koji, Suzuki, Nobuhiro, Ikedo, Koji, Kosaka, Takuo, Tsubotani, Shigetoshi, Tani, Akiyoshi, Funami, Miyuki, Amano, Michiko, Yamamoto, Yoshio, Aertgeerts, Kathleen, Yano, Jason, Maezaki, Hironobu
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetamides - chemistry amino acids Arginine - chemistry Bidentate interaction Biological and medical sciences Crystallography, X-Ray Dipeptidyl peptidase IV (DPP-4) dipeptidyl-peptidase IV Dipeptidyl-Peptidase IV Inhibitors - chemistry Dipeptidyl-Peptidase IV Inhibitors - pharmacology Drug Design General and cellular metabolism. Vitamins hydrogen bonding Medical sciences Models, Molecular niacin Pharmacology. Drug treatments Structure-Activity Relationship Structure-based drug design (SBDD) X-radiation
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