Synthesis and biological activity of novel substituted pyridines and purines containing 2,4-thiazolidinedione.
A series of substituted pyridines and purines containing 2,4-thiazolidinedione were designed and synthesized from their corresponding pyridines and purines. These synthesized compounds (entry no. 6a-d, 12a-e, 18a-d, 23a-c) were evaluated for their effect on triglyceride accumulation in 3T3-L1 cells in vitro and their hypoglycemic and hypolipidemic activity in the genetically diabetic KKA(y) mice in vivo. On the basis of their biological activities, 5-(4-[2-[N-methyl-(5-phenyl-pyridin-2-yl)amino]ethoxy]benzyl)thiazolidine-2,4-dione (6d) was selected as a candidate for further pharmacological studies.
Kim
Bok Young
BY
New Drug Research Laboratories, Chong Kun Dang Research Institute, Cheonan P.O. Box 74, Cheonan 330-831, South Korea.
Ahn
Joong Bok
JB
Lee
Hong Woo
HW
Kang
Sung Kwon
SK
Lee
Jung Hwa
JH
Shin
Jae Soo
JS
Ahn
Soon Kil
SK
Hong
Chung Il
CI
Yoon
Seung Soo
SS
D041721:3T3-L1 Cells; D000818:Animals; D001786:Blood Glucose / Q000187:drug effects; D002455:Cell Division / Q000187:drug effects; D002478:Cells, Cultured; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy*; D004195:Disease Models, Animal; D015195:Drug Design; D022781:Hepatocytes / Q000187:drug effects / Q000378:metabolism; D007004:Hypoglycemic Agents / Q000008:administration & dosage / Q000627:therapeutic use; D000960:Hypolipidemic Agents / Q000008:administration & dosage / Q000627:therapeutic use; D008297:Male; D051379:Mice; D015394:Molecular Structure; D011687:Purines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D045162:Thiazolidinediones / Q000737:chemistry*; D014280:Triglycerides / Q000378:metabolism
D001786:Blood Glucose; D007004:Hypoglycemic Agents; D000960:Hypolipidemic Agents; D011687:Purines; D011725:Pyridines; D045162:Thiazolidinediones; D014280:Triglycerides; C089946:2,4-thiazolidinedione