Application of 3-(morpholine substituted arylimido)indole compounds in the preparation of vasodilation and antihypertensive drugs
A technology of arylimine-based compounds, applied in the field of research and development of new drug candidate compounds, to achieve good vasodilation in vitro and antihypertensive activity in vivo
Active Publication Date: 2021-03-30
陕西凯诺秦康科技有限公司
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[0005] At present, there is no relevant report on the antihypertensive (vasodilation in vitro and antihypertensive activity in vivo) of the above compounds
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[0032] In order to enable those skilled in the art to better understand the solutions of the present invention, the following will clearly and completely describe the technical solutions in the embodiments of the present invention in conjunction with the drawings in the embodiments of the present invention. Obviously, the described embodiments are only It is an embodiment of a part of the present invention, but not all embodiments. Based on the embodiments of the present invention, all other embodiments obtained by persons of ordinary skill in the art without making creative efforts shall fall within the protection scope of the present invention.
[0033] It should be noted that the terms "first" and "second" in the description and claims of the present invention and the above drawings are used to distinguish similar objects, but not necessarily used to describe a specific sequence or sequence. It is to be understood that the data so used are interchangeable under appropriate ...
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The invention discloses application of 3-(morpholine substituted aromatic imino) indole compounds in preparation of vasodilator and antihypertensive drugs, and belongs to the technical field of research and development of new drug candidate compounds. Myograph is adopted to detect the in-vitro vasodilator activity of the target compounds. Results show that the 3-(morpholine substituted aromatic imino) indole compounds provided by the invention have relatively strong diastolic activity on high-potassium or PE pre-contracted in-vitro vascular rings, and T4 and T16 have the strongest vasodilatation activity. Taking T4 and T16 as examples, in-vivo antihypertensive activity of the target compounds is detected by adopting SHR. Results show that both T4 and T16 have strong in-vivo antihypertensive activity, the activity of T4 and T16 is equivalent to or better than that of captopril which is a current clinical first-line antihypertensive drug, and a reliable lead drug can be provided for antivasospastic disease and antihypertensive treatment.
Description
technical field [0001] The invention belongs to the technical field of research and development of new drug candidate compounds, and relates to the application of a 3-(morpholine-substituted arylimino) indole compound in the preparation of vasodilation and antihypertensive drugs. Background technique [0002] Cardiovascular and cerebrovascular disease is the disease with the highest incidence rate in the world, and its fatality rate and disability rate rank first among various diseases. Hypertension (Hypertension) refers to the increase of systemic arterial blood pressure (systolic blood pressure and / or diastolic blood pressure) as the main feature (systolic blood pressure ≥ 140 mmHg, diastolic blood pressure ≥ 90 mmHg) without the use of antihypertensive drugs, which may be accompanied by cardiac, Clinical syndrome of functional or organic damage to brain, kidney and other organs. According to the latest guidelines for prevention and treatment of hypertension in 2018, the ...
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IPC IPC(8): A61K31/5377A61P9/12A61P9/08
CPCA61K31/5377A61P9/08A61P9/12
Inventor 曹慧玲吴少平孟歌秦魏李慧瑾贺春霞邢露周鑫赵栋李鹏权金曦
Owner 陕西凯诺秦康科技有限公司