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首页> 外文期刊>Acta Crystallographica Section E: Crystallographic Communications >Eprosartan mesylate, an angiotensin II receptor antagonist
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Eprosartan mesylate, an angiotensin II receptor antagonist

机译:甲磺酸依普罗沙坦,血管紧张素II受体拮抗剂

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The title compound, eprosartan mesylate {systematic name: 2-butyl-1-(4-carb-oxy-benz-yl)-5-[(E)-2-carb-oxy-3-(thio-phen-2-yl)prop-1-en-yl]-1H-imidazol-3-ium methane-sulfonate}, C23H25N2O4S+·CH3O3S?, one of the angiotensin II-receptor antagonists, is effective in regulating hypertension, induced or exacerbated by angiotensin II, and in the treatment of congestive heart failure, renal failure and glaucoma. In the eprosartan residue, which appears in this crystal in the cationic imidazolium form, the benzene ring plane is almost orthogonal to that of the imidazole ring, making a dihedral angle of 87.89?(2)°. The thio-phene ring forms dihedral angles of 66.54?(2) and 67.12?(2)° with the benzene and imidazole rings, respectively. The imidazolium NH group and the H atom of the aromatic carboxyl group participate in hydrogen bonds with the the O atoms of the anion, thus forming centrosymmetric aggregates made up of two cations and two anions each. The second carboxyl group further links the above-mentioned aggregates through a conventional centrosymmetric hydrogen-bonding motif into infinite chains along [011].
机译:标题化合物甲磺酸依普罗沙坦(系统名称:2-丁基-1-(4-碳氧基-苯甲酰基)-5-[(E)-2-碳氧基-3-(硫代苯-2-) yl)prop-1-en-yl] -1H-咪唑-3-甲磺酸盐},C23H25N2O4S +·CH3O3Sα,是血管紧张素II受体拮抗剂之一,可有效调节由血管紧张素II诱发或加重的高血压,并用于治疗充血性心力衰竭,肾衰竭和青光眼。在该晶体中以阳离子咪唑形式出现的依普罗沙坦残基中,苯环平面几乎与咪唑环的平面正交,二面角为87.89°(2)°。噻吩环与苯环和咪唑环分别形成66.54θ(2)和67.12θ(2)°的二面角。咪唑鎓的NH基团和芳族羧基的H原子与阴离子的O原子参与氢键,从而形成由两个阳离子和两个阴离子组成的中心对称聚集体。第二个羧基通过常规的中心对称氢键基团进一步将上述聚集体连接成沿[011]的无限链。

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