title: Molecular design, synthesis, and hypoglycemic and hypolipidemic activities of novel pyrimidine derivatives having thiazolidinedione.
abstract: 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.
authors.affiliation: New Drug Research Laboratories, Chong Kun Dang Research Institute, Cheonan P.O. Box 74, Cheonan 330-831, South Korea. hwlee@ckdpharm.com
authors.forename: Hong Woo
authors.initials: HW
authors.lastname: Lee
authors.forename: Bok Young
authors.initials: BY
authors.lastname: Kim
authors.forename: Joong Bok
authors.initials: JB
authors.lastname: Ahn
authors.forename: Sung Kwon
authors.initials: SK
authors.lastname: Kang
authors.forename: Jung Hwa
authors.initials: JH
authors.lastname: Lee
authors.forename: Jae Soo
authors.initials: JS
authors.lastname: Shin
authors.forename: Soon Kil
authors.initials: SK
authors.lastname: Ahn
authors.forename: Sang Joon
authors.initials: SJ
authors.lastname: Lee
authors.forename: Seung Soo
authors.initials: SS
authors.lastname: Yoon
mesh_terms: 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*
chemical_list: D007004:Hypoglycemic Agents; D000960:Hypolipidemic Agents; D011743:Pyrimidines; D045162:Thiazolidinediones; D000077154:Rosiglitazone; D000077205:Pioglitazone