Synthesis and evaluation of some novel dibenzo(b,d)furan carboxylic acids as potential anti-diabetic agents.

Lakshminarayana N; Prasad YR; Gharat L; Thomas A; Narayanan S; Raghuram A; Srinivasan CV; Gopalan B

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Synthesis and evaluation of some novel dibenzo(b,d)furan carboxylic acids as potential anti-diabetic agents.

机译：某些新型二苯并（b，d）呋喃羧酸作为潜在的抗糖尿病药的合成与评价。

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A series of novel dibenzo[b,d]furan mono-carboxylic acid derivatives were synthesized, characterized and evaluated for their ability to inhibit Protein Tyrosine Phosphatase 1B (PTP1B) in vitro in order to use them as potential anti-diabetic agents. Structure-activity relationship study led to the identification of potent compound 5 E which inhibited PTP1B with IC(50) value of 82+/-0.43 nM. Compound 5 E was screened in vivo as drug candidate for anti-diabetic activity using rosiglitazone maleate as the standard. Compound 5 E showed significant reduction in body weight, fed-state whole blood glucose (WBG), fasting WBG, plasma glucose and plasma cholesterol levels and non-significant reduction in fasting plasma triglyceride levels in ob/ob mice.

机译：合成，表征和评估了其在体外抑制蛋白酪氨酸磷酸酶1B（PTP1B）的能力，以此系列新型二苯并[b，d]呋喃单羧酸衍生物，以用作潜在的抗糖尿病药。结构-活性关系研究导致鉴定出有效化合物5 E，该化合物抑制PTP1B，IC（50）值为82 +/- 0.43 nM。使用马来酸罗格列酮作为标准品，体内筛选化合物5 E作为抗糖尿病活性的候选药物。化合物5 E在ob / ob小鼠中显示出体重，进食状态全血糖（WBG），空腹WBG，血浆葡萄糖和血浆胆固醇水平显着降低，并且空腹血浆甘油三酯水平显着降低。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2010年第9期|共10页
作者
Lakshminarayana N; Prasad YR; Gharat L; Thomas A; Narayanan S; Raghuram A; Srinivasan CV; Gopalan B;
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正文语种 eng
中图分类医药、卫生;劳动卫生;
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1. Synthesis and evaluation of some novel dibenzo(b,d)furan carboxylic acids as potential anti-diabetic agents. [J] . Lakshminarayana N, Prasad YR, Gharat L, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2010,第9期

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Synthesis and evaluation of some novel dibenzo(b,d)furan carboxylic acids as potential anti-diabetic agents.

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