Targeting PPAR<i>γ</i>Receptor Using New Phosphazene Derivative Containing Thiazolidinedione: Design, Synthesis, and Glucose Uptake
Targeting PPAR<i>γ</i>Receptor Using New Phosphazene Derivative Containing Thiazolidinedione: Design, Synthesis, and Glucose Uptake作者机构：Department of Chemistry College of Science UAE University Al-Ain UAE Department of Pharmacology College of Health and Science UAE University Al-Ain UAE
出 版 物：《Open Journal of Medicinal Chemistry》 (药物化学期刊（英文）)
年 卷 期：2020年第10卷第2期
页 面：35-45页
学科分类：1002[医学-临床医学] 100201[医学-内科学(含：心血管病、血液病、呼吸系病、消化系病、内分泌与代谢病、肾病、风湿病、传染病)] 10[医学]
主 题：Type 2 Diabetes PPARs TZD Compound Cyclotriphosphazene
摘 要：The peroxisome proliferator activator receptor-γ (PPAR-γ) remained the most effective target for management of diabetes mellitus. The present work endeavors rational designing new PPAR-γ 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 PPARγ 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 PPARγ agonist. The in-vitro antidiabetic activity showed that compound 8 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.
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