Sławik T
Lehrstuhl für Pharmazeutische Chemie, Pharmazeutische Fakultät, Medizinischen Akademie Lublin, Polen.
Pharmazie. 1991 Nov;46(11):777-80.
In the search for pharmacological active new derivatives of 1,2-benzisothiazolin-3-on amides of (3-oxo-1,2-benzisothiazolin-2-yl)acetic acid and 3-(3-oxo-1,2-benzisothiazolin-2-yl)propionic acid were obtained. In the reaction of these amides with formaldehyde and various second aryl amines the title compounds are formed. Morpholinmethylamide of (3-oxo-1,2-benzisothiazolin-2-yl)acetic acid showed activity against Trichomonas vaginalis. In the reaction of ethyl esters of (3-oxo-1,2-benzisothiazolin-2-yl) acetic- and -propionic acids with hydrazine hydrate products of ring-opening of isothiazole-2,2'-dithio-bis [N- (ethoxycarbonylmethyl)benzamide] and 2,2'-dithio-bis[N-(ethoxycarbonylethyl)benzamide are formed.
在寻找1,2 - 苯并异噻唑啉 - 3 - 酮酰胺类具有药理活性的新衍生物过程中,获得了(3 - 氧代 - 1,2 - 苯并异噻唑啉 - 2 - 基)乙酸和3 - (3 - 氧代 - 1,2 - 苯并异噻唑啉 - 2 - 基)丙酸的酰胺。在这些酰胺与甲醛及各种二级芳胺的反应中,形成了标题化合物。(3 - 氧代 - 1,2 - 苯并异噻唑啉 - 2 - 基)乙酸的吗啉甲基酰胺对阴道毛滴虫显示出活性。在(3 - 氧代 - 1,2 - 苯并异噻唑啉 - 2 - 基)乙酸乙酯和丙酸乙酯与水合肼的反应中,形成了异噻唑 - 2,2'- 二硫代 - 双[N - (乙氧羰基甲基)苯甲酰胺]和2,2'- 二硫代 - 双[N - (乙氧羰基乙基)苯甲酰胺]的开环产物。