Journal
CLINICAL AND EXPERIMENTAL HYPERTENSION
Volume 38, Issue 5, Pages 435-442Publisher
TAYLOR & FRANCIS INC
DOI: 10.3109/10641963.2016.1151527
Keywords
Antihypertension; AT(1) antagonists; 5-oxo-1; -oxadiazole; N-phenyl indole; acute toxicity
Funding
- Foundation of Science and Technology Commission of Shanghai [13431900700, 14431906200]
- Foundation of Donghua University [14D110906]
- Foundation of Ningbo Science & Technology Bureau [2015A610274]
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A series of new 5-oxo-1,2,4-oxadiazole derivatives with 1, 4-disubsituted or 1, 5-disubsituted indole group was designed, synthesized, and pharmacologically evaluated. These derivatives displayed high affinities to the AT(1) receptor at the same order of magnitude to losartan. The methyl ester with 1, 4-disubsituted indole group, 1 (5.01 +/- 1.67 nM) showed high antihypertension activity on spontaneously hypertensive rats (SHRs). Its maximal response lowered 30 mmHg of mean blood pressure (MBP) at 10 mg/kg after oral administration, which was better than irbesartan, and the antihypertensive effect lasted beyond 24 h. These results made 1 deserve further investigation.
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