非肽类血管紧张素 II 受体拮抗剂：N-[(苄氧基)苄基]咪唑及相关化合物作为强效抗高血压药物。
Nonpeptide angiotensin II receptor antagonists: N-[(benzyloxy)benzyl]imidazoles and related compounds as potent antihypertensives.
作者信息
Carini D J, Duncia J V, Johnson A L, Chiu A T, Price W A, Wong P C, Timmermans P B
机构信息
Medicinal Chemistry Section, E. I. du Pont de Nemours and Co., Inc., Wilmington, Delaware 19880.
出版信息
J Med Chem. 1990 May;33(5):1330-6. doi: 10.1021/jm00167a008.
A series of compounds has been synthesized and demonstrated to be antagonists of the angiotensin II (AII) receptor. These compounds are structurally related to the N-(benzamidobenzyl)imidazoles and extend the scope of this new class of nonpeptide AII antagonists. It has been found that the amide linkage (X = NHCO) in the N-(benzamidobenzyl)imidazoles can be replaced successfully by a variety of groups (X = single bond, O, S, CO, OCH2, CH = CH, NHCONH); linkers of 0-1 atoms in length are most effective. When administered intravenously to awake renal hypertensive rats, these compounds are potent antihypertensives.
已合成了一系列化合物，并证明它们是血管紧张素 II（AII）受体的拮抗剂。这些化合物在结构上与 N -（苯甲酰胺苄基）咪唑有关，并扩展了这类新型非肽 AII 拮抗剂的范围。已发现 N -（苯甲酰胺苄基）咪唑中的酰胺键（X = NHCO）可以被多种基团（X = 单键、O、S、CO、OCH2、CH = CH、NHCONH）成功取代；长度为 0 - 1 个原子的连接基最有效。当给清醒的肾性高血压大鼠静脉注射这些化合物时，它们是强效降压药。
Zotero 插件