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    • 1. 发明授权
    • Thiazolidine derivatives with antibiotic activity
    • 具有抗生素活性的噻唑烷衍生物
    • US4405618A
    • 1983-09-20
    • US279454
    • 1981-07-01
    • Michele Di SchienaVittoria Orru
    • Michele Di SchienaVittoria Orru
    • A61K31/43A61K31/545A61K31/546A61P31/04C07D499/00C07D499/76C07D501/20C07D501/24C07D501/26C07D501/34C07D501/38C07D501/46C07D501/57
    • C07D501/20C07D499/00C07D501/57
    • New derivatives of 1,3-thiazolidin-4-yl carboxylic acid of the general formula I ##STR1## wherein R represents hydrogen, (C.sub.1 -.sub.4)alkyl, aralkyl, phenyl, phenyl substituted by a halogen atom or a methoxy group, formyl, acyl, trimethylsilyl;R' represents hydrogen, a pharmaceutically acceptable inorganic or organic cation, (C.sub.1 -.sub.4)alkyl, 2,2,2-trichloroethyl, acetonyl, benzyl, benzyl substituted by nitro or methoxy, phenyl, nitrophenyl, benzhydryl or trimethylsilyl;R' may also represent a radical capable of providing metabolic activation in vivo selected from acetoxymethyl, pivaloyloxymethyl, phthalidyl, benzoyloxymethyl, 5-indanyl, a group of formula ##STR2## or a group of formula ##STR3## in which R" stands for (C.sub.1 -.sub.4)alkyl, (C.sub.5 -.sub.6)cycloalkyl or aryl; A represents hydrogen, halogen, N.sub.3, OH, NH.sub.2 ; or a quaternary N-atom, particularly ##STR4## (and in this case R' is a negative charge; or a O--CO--NH.sub.2 group; or a group of the formula OR"'; O--COR"', NH--CO--R"' or SR"', where R"' is (C.sub.1 -C.sub.4)alkyl, aryl, substituted aryl or a heterocyclic group which can carry lower alkyls;n may be zero or 1.The compounds possess antibacterial utility against microbial infections in man, animals and plants.
    • 通式I(I)的1,3-噻唑烷-4-基羧酸的新衍生物其中R表示氢,(C 1-4)烷基,芳烷基,苯基,被卤素原子取代的苯基或甲氧基 基,甲酰基,酰基,三甲基甲硅烷基; R'表示氢,药学上可接受的无机或有机阳离子,(C 1-4)烷基,2,2,2-三氯乙基,丙酰基,苄基,被硝基或甲氧基取代的苄基,苯基,硝基苯基,二苯甲基或三甲基甲硅烷基; R'也可以代表能够在体内提供代谢活化的基团,其选自乙酰氧基甲基,新戊酰氧基甲基,邻苯二甲酰基,苯甲酰氧基甲基,5-二氢化茚基,式为“IMAGE”或式“IMAGE”的一组,其中R“ (C 1-4)烷基,(C 5-6)环烷基或芳基; A表示氢,卤素,N 3,OH,NH 2; 或季氮原子,特别是(在这种情况下,R'为负电荷;或O-CO-NH 2基团;或式OR“'的基团; O-COR” NH-CO-R“'或SR”',其中R“是(C 1 -C 4)烷基,芳基,取代的芳基或可带有低级烷基的杂环基; n可以是0或1.化合物 在人类,动物和植物中具有抵抗微生物感染的抗菌效果。