کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10585521 | 981367 | 2012 | 15 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and biological evaluation of novel potent angiotensin II receptor antagonists with anti-hypertension effect
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Synthesis and biological evaluation of novel potent angiotensin II receptor antagonists with anti-hypertension effect Synthesis and biological evaluation of novel potent angiotensin II receptor antagonists with anti-hypertension effect](/preview/png/10585521.png)
چکیده انگلیسی
A series of novel angiotensin II type 1 receptor antagonists were prepared. Radioligand binding assay suggested that compounds 1b and 1c could be recognized by the AT1 receptor with an IC50 value of 1.6 ± 0.09 nM and 2.64 ± 0.7 nM, respectively. In vivo anti-hypertension experiments showed that compounds (1a, 1b, 1c, 1e) elicited a significant decrease in SBP and DBP of spontaneous hypertensive rats (SHRs). The antihypertensive effects maintained for 10 h, which indicated that these compounds had a favorable blood pressure-lowering effect. Acute toxicity testing suggested that the LD50 value of compound 1b was 2316.8 mg/kg which was lower than valsartan (LD50 = 307.50 mg/kg) but higher than losartan (LD50 = 2248 mg/kg). So they could be considered as novel anti-hypertension candidates and deserved for further investigation.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 8, 15 April 2012, Pages 2747-2761
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 8, 15 April 2012, Pages 2747-2761
نویسندگان
Yong-yan Nie, Ya-jing Da, Hao Zheng, Xiao-xia Yang, Lin Jia, Cai-hong Wen, Li-sha Liang, Juan Tian, Zhi-long Chen,