摘要:
Novel cephem compounds of the general formula : wherein R¹ is a lower alkyl group, and salts and esters thereof, showing excellent and balanced antibacterial activity against a broad spectrum of bacteria, especially by rectal administration, and their production and use as antimicrobial agents are described.
摘要:
A compound of the formula; wherein R 1 is an amino group which may be protected, R 3 is a hydrogen atom or an optionally substituted hydrocarbon residue; Z is S, S → O, O or CH 2 , R 4 is a hydrogen atom, methoxy group or formamido group, R 13 is a hydrogen atom, methyl group, hydroxyl group or halogen atom and A⊕ is an optionally substituted imidazolium-1-yl group forming a condensed ring at the 2,3- or 3,4-position or a pharmaceutically acceptable salt or ester thereof is novel and has excellent antibacterial activity.
摘要:
A compound of the formula; wherein R° stands for hydrogen atom, nitrogen-containing heterocyclic group, acyl group or esterified carboxyl group. Z stands for S , S→-O, 0 or CH 2 , R' stands for hydrogen atom. methoxy group or formamido group, R 13 stands for hydrogen atom. methyl group, hydroxyl group or halogen atom and A stands for an optionally substituted imidazol-1-yl group forming a condensed ring at the 2.3- or 3.4-position or a physiologically or phamaceutically acceptable salt or ester thereof. This compound is novel and has excellent antibacterial activity.
摘要:
A compound of the formula; wherein R 1 is an amino group which may be protected, R 3 is a hydrogen atom or an optionally substituted hydrocarbon residue; Z is S, S → O, O or CH 2 , R 4 is a hydrogen atom, methoxy group or formamido group, R 13 is a hydrogen atom, methyl group, hydroxyl group or halogen atom and A⊕ is an optionally substituted imidazolium-1-yl group forming a condensed ring at the 2,3- or 3,4-position or a pharmaceutically acceptable salt or ester thereof is novel and has excellent antibacterial activity.
摘要:
1-lodoalkyl acylates, which are useful as raw materials for the esterification of cephalosporins and penicillins, are prepared in a high degree of purity and in high yield by reacting a carboxylic acid iodide with an aldehyde. The carboxylic acid iodide may be prepared in situ by reacting a carboxylic acid chloride with a salt of hydriodic acid and then reacting the resulting product with an aldehyde, or by simultaneously reacting a carboxylic acid chloride, a salt of hydriodic acid I and an aldehyde with one another.
摘要:
A compound of the formula wherein (1) R 1 is a lower alkyl group of 2 to 6 carbon atoms or a cycloalkyl group of 5 to 7 carbon atoms and R 2 is a cycloalkyl group of 5 to 7 carbon atoms or a lower alkyl group of 1 to 3 carbon atoms which is substituted by a cycloalkyl group of 5 to 7 carbon atoms or by a phenyl group, or (2) R, is a cycloalkyl group of 5 to 7 carbon atoms and R 2 is a lower alkyl group of 1 to 5 carbon atoms, or a pharmaceutically acceptable salt thereof, processes for preparing the same and a pharmaceutical composition thereof are provided. The compound can orally be applied as antibiotics having improved bioavailability.
摘要:
A cephem compound of the formula: wherein R, is an optionally protected amino group; Q is a nitrogen atom or a C-R 2 group; R 2 is a hydrogen or halogen atom; R 3 is a hydrogen atom or a hydrocarbon residue which may be substituted; R 4 is a hydrogen atom or a methoxy group; R 5 is a nitrogen-containing aromatic heterocyclic group which may be substituted; A denotes that further substituted or substituents may be present on the pyridine ring; n is 0 or 1 or a physiologically or pharmaceutically acceptable salt or ester thereof. This compound is novel and has an excellent antibacterial activity.
摘要:
1-lodoalkyl acylates, which are useful as raw materials for the esterification of cephalosporins and penicillins, are prepared in a high degree of purity and in high yield by reacting a carboxylic acid iodide with an aldehyde. The carboxylic acid iodide may be prepared in situ by reacting a carboxylic acid chloride with a salt of hydriodic acid and then reacting the resulting product with an aldehyde, or by simultaneously reacting a carboxylic acid chloride, a salt of hydriodic acid I and an aldehyde with one another.
摘要:
1-Sulfo-2-azetidinone derivative of the formula: wherein
R 1 is an amino group which may optionally be acylated or protected; and R 2 is a five- or six-membered ring-forming primary or secondary amido group which may contain at least one of nitrogen, sulfur and oxygen atoms as a ring-constituting element; or a pharmaceutically acceptable salt thereof, is novel and possesses excellent antimicrobial activity and b-lactamase inhibitory activity, and is useful as a treatment agent against infections in man and mammals.
摘要翻译:1-磺基-2-氮杂环丁酮衍生物,其结构式为:CHEM,其中R 1是任选被酰化或保护的氨基; R 2是可以含有氮,硫和氧原子中的至少一个作为构成环的元素的五元或六元环形的伯或仲酰胺基; 或其药学上可接受的盐是新颖的并且具有优异的抗微生物活性和β-内酰胺酶抑制活性,并且可用作抗人和哺乳动物感染的治疗剂。