Nazreen Syed, Alam Mohammad Sarwar, Hamid Hinna, Yar Mohammad Shahar, Shafi Syed, Dhulap Abhijeet, Alam Perwez, Pasha M A Q, Bano Sameena, Alam Mohammad Mahboob, Haider Saqlain, Ali Yakub, Kharbanda Chetna, Pillai K K
Department of Chemistry, Faculty of Science, Jamia Hamdard (Hamdard University), New Delhi 110 062, India.
Department of Chemistry, Faculty of Science, Jamia Hamdard (Hamdard University), New Delhi 110 062, India.
Eur J Med Chem. 2014 Nov 24;87:175-85. doi: 10.1016/j.ejmech.2014.09.010. Epub 2014 Sep 16.
A library of novel 1,3,4-oxadiazole and 2-4-thiazolidinedione based bis-heterocycles 7 (a-r) has been synthesized which exhibited significant PPAR-γ transactivation and blood glucose lowering effect comparable with the standard drugs Pioglitazone and Rosiglitazone. Compounds 7m and 7r did not cause body weight gain and were found to be free from hepatotoxic and cardiotoxic side effects. Compounds 7m and 7r increased PPAR-γ gene expression by 2.10 and 2.00 folds, respectively in comparison to the standard drugs Pioglitazone (1.5 fold) and Rosiglitazone (1.0 fold). Therefore the compounds 7m and 7r may be considered as potential candidates for development of new antidiabetic agents.
已合成了一系列基于新型1,3,4-恶二唑和2,4-噻唑烷二酮的双杂环化合物7（a - r），这些化合物表现出显著的过氧化物酶体增殖物激活受体γ（PPAR - γ）反式激活作用和降血糖效果，与标准药物吡格列酮和罗格列酮相当。化合物7m和7r不会导致体重增加，且无肝毒性和心脏毒性副作用。与标准药物吡格列酮（1.5倍）和罗格列酮（1.0倍）相比，化合物7m和7r分别使PPAR - γ基因表达增加2.10倍和2.00倍。因此，化合物7m和7r可被视为开发新型抗糖尿病药物的潜在候选物。
