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    • 6. 发明授权
    • 6-(Hydroxyethyl)-2-[(heterocyclyl or
aryl)thioalkylthio]-penem-3-carboxylates
    • 6-(羟乙基)-2 - [(杂环基或芳基)硫代烷硫基] - 丙烯-3-羧酸酯
    • US4431654A
    • 1984-02-14
    • US365427
    • 1982-04-05
    • Viyyoor M. GirijavallabhanAshit K. GangulyNaginbhai M. PatelYi-Tsung Liu
    • Viyyoor M. GirijavallabhanAshit K. GangulyNaginbhai M. PatelYi-Tsung Liu
    • C07D499/88C07D499/00A61K31/425
    • C07D499/88
    • There are disclosed antibacterially effective compounds represented by the formula ##STR1## wherein R.sub.2 represents a substituted or unsubstituted single ring or double fused ring aryl or heterocyclyl radical bonded to the sulfur atom by a ring carbon, selected from the group consisting of phenyl, naphthyl, benzothiazolyl, oxazinyl, pyridyl, purinyl, imidazolyl, pyrryl, thiazolyl, thiadiazolyl, benzimidazolyl, triazinyl, furyl, thienyl, thiazinyl, triazolyl, tetrazolyl and pyrimidyl, wherein when substituted, said aryl or heterocyclic rings have one or more substituent which can be the same or different(a) are on a ring carbon or heteroatom, and are independently selected from the group consisting of lower alkyl, ##STR2## and loweralkylene ##STR3## wherein R.sub.4 and R.sub.5 are the same or different and are independently selected from the group consisting of hydrogen, halogen and lower alkyl or(b) are on a ring carbon atom only and are selected from the group consisting of .dbd.O, hydroxy, lower alkoxy, --COOR.sub.3 or halogen; wherein R.sub.3 represents hydrogen, a pharmaceutically acceptable readily metabolizable ester-forming substituent or a pharmaceutically acceptable cation, and the wavy line represents the 5R,6S,8R and 5R,6R,8S stereoisomers; and novel intermediates, processes and antibacterial pharmaceutical and veterinary compositions thereof.
    • 公开了由下式表示的抗菌有效化合物,其中R 2表示取代或未取代的单环或双稠环芳基或杂环基,其通过环碳与硫原子键合,所述环碳选自苯基,萘基 苯并噻唑基,恶嗪基,吡啶基,嘌呤基,咪唑基,吡咯基,噻唑基,噻二唑基,苯并咪唑基,三嗪基,呋喃基,噻吩基,噻嗪基,三唑基,四唑基和嘧啶基。其中当被取代时,所述芳基或杂环具有一个或多个取代基, 相同或不同的(a)在环碳或杂原子上,并且独立地选自低级烷基,低级亚烷基和低级亚烷基,其中R 4和R 5相同或不同,并且独立地选自 由氢,卤素和低级烷基组成的基团或(b)仅在环碳原子上,并且选自= O,羟基,低级 烷氧基,-COOR 3或卤素; 其中R3表示氢,药学上可接受的易代谢的酯形成取代基或药学上可接受的阳离子,波浪线表示5R,6S,8R和5R,6R,8S立体异构体; 及其新型中间体,方法和抗菌药物和兽药组合物。