新型2-芳基萘并[1,2-d]恶唑衍生物作为具有抗高血糖活性的潜在蛋白酪氨酸磷酸酶-1B抑制剂。
Novel 2-aryl-naphtho[1,2-d]oxazole derivatives as potential PTP-1B inhibitors showing antihyperglycemic activities.
作者信息
Kumar Atul, Ahmad Pervez, Maurya Ram Awatar, Singh A B, Srivastava Arvind K
机构信息
Medicinal and Process Chemistry Division, Central Drug Research Institute, P.O. Box 172, Lucknow 226001, Uttar Pradesh, India.
出版信息
Eur J Med Chem. 2009 Jan;44(1):109-16. doi: 10.1016/j.ejmech.2008.03.009. Epub 2008 Mar 27.
A series of 2-aryl-naphtho[1,2-d]oxazole derivatives have been synthesized and evaluated for PTP-1B inhibitory activity. The compounds have been screened in vivo for antidiabetic activity under sucrose loaded model (SLM), sucrose-challenged streptozotocin-induced diabetic rat model (STZ-S) and db/db mice model. Compounds 8 and 12 have shown promising PTP-1B inhibitory activity, significant antidiabetic activity, moderate lipid and triglyceride lowering activity.
已合成了一系列2-芳基萘并[1,2-d]恶唑衍生物，并对其蛋白酪氨酸磷酸酶-1B（PTP-1B）抑制活性进行了评估。这些化合物已在体内蔗糖负荷模型（SLM）、蔗糖激发的链脲佐菌素诱导糖尿病大鼠模型（STZ-S）和db/db小鼠模型中进行了抗糖尿病活性筛选。化合物8和12表现出有前景的PTP-1B抑制活性、显著的抗糖尿病活性以及适度的降血脂和降甘油三酯活性。
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