Molecular design, synthesis, and hypoglycemic and hypolipidemic activities of novel pyrimidine derivatives having thiazolidinedione.
We previously reported the synthesis and biological activity of novel substituted pyridines and purines having thiazolidinedione with hypoglycemic and hypolipidemic activities. We now report the synthesis and antidiabetic activity of novel substituted pyrimidines having thiazolidinedione moiety. These compounds (entry No. 5a-i, 10a-d and 16) were evaluated for their glucose and lipid lowering activity in KKA(y) mice. From the results, novel compounds, 5c and 5g, exhibited considerably more potent biological activity than that of the reference compounds, pioglitazone and rosiglitazone, respectively.
Lee
Hong Woo
HW
New Drug Research Laboratories, Chong Kun Dang Research Institute, Cheonan P.O. Box 74, Cheonan 330-831, South Korea. hwlee@ckdpharm.com
Kim
Bok Young
BY
Ahn
Joong Bok
JB
Kang
Sung Kwon
SK
Lee
Jung Hwa
JH
Shin
Jae Soo
JS
Ahn
Soon Kil
SK
Lee
Sang Joon
SJ
Yoon
Seung Soo
SS
D000818:Animals; D002460:Cell Line; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D007004:Hypoglycemic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000960:Hypolipidemic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008297:Male; D051379:Mice; D008817:Mice, Mutant Strains; D008956:Models, Chemical; D000077205:Pioglitazone; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D000077154:Rosiglitazone; D045162:Thiazolidinediones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
D007004:Hypoglycemic Agents; D000960:Hypolipidemic Agents; D011743:Pyrimidines; D045162:Thiazolidinediones; D000077154:Rosiglitazone; D000077205:Pioglitazone