Bozdağ-Dündar Oya, Verspohl Eugen J, Waheed Abdul, Ertan Rahmiye
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, Tandoğan, Ankara, Turkey.
Arzneimittelforschung. 2003;53(12):831-6. doi: 10.1055/s-0031-1299837.
A new series of furochromone-2,4-thiazolidinedione derivatives (VIIa-h) was prepared by Knoevenagel reaction of substituted-2,4-thiazolidinediones (VIa-h) with Khellin-2-carboxaldehyde (IV). The prepared compounds were tested for their insulinotropic activities in INS-1 cells. Compounds VIId and VIIf (at lower concentration; 1 microgram/ml) were able to increase insulin release in the presence of 5.6 mmol/l glucose. Both these compounds (VIId and VIIf) and VIIg increased glucose uptake in NIH-3T3 cells. Thus these 3 compounds should be tested for antidiabetic effects in vivo.
通过取代的2,4 - 噻唑烷二酮(VIa - h)与凯林 - 2 - 甲醛(IV)的克诺文纳盖尔反应制备了一系列新的呋喃色酮 - 2,4 - 噻唑烷二酮衍生物(VIIa - h)。对所制备的化合物在INS - 1细胞中进行促胰岛素分泌活性测试。化合物VIId和VIIf(在较低浓度;1微克/毫升)能够在5.6毫摩尔/升葡萄糖存在的情况下增加胰岛素释放。这两种化合物(VIId和VIIf)以及VIIg均增加了NIH - 3T3细胞中的葡萄糖摄取。因此,应对这3种化合物进行体内抗糖尿病作用测试。