Insulin-releasing activity of a series of phenylalanine derivatives

• Published in: European journal of medicinal chemistry Vol. 43; no. 9; pp. 1997 - 2003
• Main Authors: Tang, Lei, Yu, Juanhong, Wu, Haoshu, Fan, Houxing, Yang, Yushe, Ji, Ruyun
• Format: Journal Article
• Language: English
• Published: ISSY-LES-MOULINEAUX Elsevier Masson SAS 01.09.2008; Elsevier
• Subjects: Animals; Biological and medical sciences; Cell Line; Chemistry, Medicinal; Cricetinae; Drug Design; General and cellular metabolism. Vitamins; Hypoglycemia effect; Hypoglycemic Agents - chemistry; Hypoglycemic Agents - pharmacology; Insulin - metabolism; Insulin-releasing activity; Insulin-sensitizing activity; Life Sciences & Biomedicine; Medical sciences; Mice; Pharmacology & Pharmacy; Pharmacology. Drug treatments; Phenylalanine; Phenylalanine - analogs & derivatives; Phenylalanine - pharmacology; Science & Technology; Hypoglycemia effect; Insulin-releasing activity; Insulin-sensitizing activity; Phenylalanine; ORAL HYPOGLYCEMIC AGENTS; COMPLICATIONS; Pancreatic hormone; Ether; Rat; Rodentia; Oral administration; In vitro; Insulin; Protein hormone; In vivo; α-Aminoacid; Vertebrata; Hypoglycemic agent; Mammalia; Structure activity relation; Animal; Enantiomer; Chemical synthesis; Oxazole derivatives; Release; Oxygen nitrogen heterocycle
• ISSN: 0223-5234; 1768-3254
• DOI: 10.1016/j.ejmech.2007.11.018

A series of phenylalanine derivatives were synthesized and their biological activities were evaluated. Compounds ( S)- 3 and ( R)- 3 exhibited more potent insulin-releasing activity than that of nateglinide, compound ( S)- 3 also showed insulin-sensitizing activity in vitro. Both compounds were tested for hypoglycemia effect in vivo. [Display omitted]