The peroxisome proliferator activator receptor-<em>γ</em> (PPAR-<em>γ</em>) remained the most effective target for management of diabetes mellitus. The present work endeavors rational designi...The peroxisome proliferator activator receptor-<em>γ</em> (PPAR-<em>γ</em>) remained the most effective target for management of diabetes mellitus. The present work endeavors rational designing new PPAR-<em>γ</em> agonist bearing cyclotriphosphazene and thiazolidine-2,4-dione scaffolds. Thiazolidinedione (TZD) derivatives are the novel class of oral antidiabetic drugs which are selective agonist for the nuclear PPAR<em>γ</em> that enhances the transcription of several insulin responsive genes but TZDs are known to cause weight gain, hepatotoxicity and fluid retention. So, cyclotriphosphazene containing thiazolidine-2,4-dione was designed, synthesized as PPAR<em>γ</em> agonist. The <em>in-vitro</em> antidiabetic activity showed that compound <strong>8</strong> has similar activity and exhibited higher glucose uptake in comparison to pioglitazone as reference drugs. This research opened new avenues for smart designing of molecules with high efficiency towards the management of hyperglycemia.展开更多
文摘The peroxisome proliferator activator receptor-<em>γ</em> (PPAR-<em>γ</em>) remained the most effective target for management of diabetes mellitus. The present work endeavors rational designing new PPAR-<em>γ</em> agonist bearing cyclotriphosphazene and thiazolidine-2,4-dione scaffolds. Thiazolidinedione (TZD) derivatives are the novel class of oral antidiabetic drugs which are selective agonist for the nuclear PPAR<em>γ</em> that enhances the transcription of several insulin responsive genes but TZDs are known to cause weight gain, hepatotoxicity and fluid retention. So, cyclotriphosphazene containing thiazolidine-2,4-dione was designed, synthesized as PPAR<em>γ</em> agonist. The <em>in-vitro</em> antidiabetic activity showed that compound <strong>8</strong> has similar activity and exhibited higher glucose uptake in comparison to pioglitazone as reference drugs. This research opened new avenues for smart designing of molecules with high efficiency towards the management of hyperglycemia.
