摘要:
Derivatives of 4,5-di(hydroxymethyl)-2-oxo-1,3-dioxole in which one hydroxy group has been esterified through the carboxy group of ampicillin or amoxicillin, and the other hydroxy group has been esterified through the carboxy group of sulbactam (penicillanic acid 1,1-dioxide), are useful as antibacterial agents. Certain novel compounds, which are useful as intermediates to the aforesaid antibacterial agents, are also disclosed.
摘要:
Compounds of the formula wherein R 1 is H or HO; Y and Z are each Cl, Br or I, or Y is H and Z is Cl, Br or I; Q is N 3 or NHCO 2 CH 2 C 6 H 4 R 4 where R 4 is H, Cl, Br, N0 2 , CH 3 or OCH 3 ; a process for their use in production of the valuable antibacterial agents 1,1-dioxopenicillanoyloxymethyl 6-(2-amino-2-phenyl- acetamido)penicillanate and 1,1-dioxopenicillanoyloxymethyl 6-[2-amino-2-(p-hydroxyphenyl)acetamido]-penicillanate, by catalytic hydrogenation in the presence of a noble metal catalyst and novel intermediates useful in preparing said compounds of formula (1).
摘要翻译:式CHEM的化合物,其中R 1是H或HO; Y和Z各自为Cl,Br或I,或Y为H,Z为Cl,Br或I; Q是N 3或NHCO 2 CH 2 C 6 H 4 R 4,其中R 4是H,Cl,Br,NO 2,CH 3或OCH 3; 它们用于生产有价值的抗菌剂6-(2-氨基-2-苯基乙酰氨基)青霉素的1,1-二氧代青霉酰氨基甲酰基和6- [2-氨基-2-(对羟基苯基)乙酰氨基的1,1-二氧代青霉烷酰氧基甲基 ]青霉烷,在贵金属催化剂存在下通过催化氢化和用于制备所述式(I)化合物的新型中间体。
摘要:
Novel pharmaceutically useful derivatives of selected known bio-affecting carboxylic acids and a process for preparing them are disclosed, said derivatives having the structural formula wherein R,, R 2 , X and X' are e.g. hydrogen, or C 1 -C 5 alkyl; and R-COO- is the acyloxy residue of:
(a) a monocarboxylic acid, e.g. indomethacin; (b) a steroidal monocarboxylic acid; (c) a cephalosporin antibiotic having one carboxylic acid function; (d) a penicillin antibiotic having one carboxylic acid function; or (e) y-aminobutyric acid, captopril or valproic acid; or having the structural formula wherein -OOC-R'-COO- is the di(acyloxy) residue of: (a) A cephalosporin antibiotic having two carboxylic acid functions; (b) a penicillin antibiotic having two carboxylic acid functions; or (c) the dicarboxylic acid, methotrexate.
Non-toxic pharmaceutically acceptable acid addition salts, N-oxides and quaternary ammonium salts of the compounds of formulas (I) and (II) are also disclosed.
摘要:
Compounds or their salts having general formulas (I) and (II): wherein s is and integer equal to 1 or 2, preferably s = 2; A is the radical of a drug and is such as to meet the pharmacological tests reported in the description, C and C1 are two bivalent radicals. The precursors of the radicals B and B1 are such as to meet the pharmacological test reported in the description.
摘要:
A pharmaceutical compound which comprises reacting the sodium penicillanic acid 1,1-dioxides with chloroiodomethane in the presence of a solvent to produce chloromethylpenicillanate 1,1-dioxides, reacting the chloromethylpenicillanate 1,1-dioxides with a sodium iodide to produce iodomethylpenicillanate 1,1-dioxides, and reacting the iodomethylpenicillanate 1,1-dioxide with sodium methampicillin and is effective in the treatment of bacterial infections in a mammal.
摘要:
Disclosed are an optically active, ethylenically unsaturated monomer represented by the following structural formula: wherein: A stands for S, SO or SO₂; X and Y each stand for a hydrogen atom or a substituent selected from the group consisting of alkyl groups and acyl groups; Z stands for a substituent selected from the group consisting of alkoxy, alkylamino, hydroxyl and silyloxy groups; and X and Y can be bonded together to form a ring with the nitrogen atom to which they are bonded or X and Y can be a single group bonded to said nitrogen atom through a double bond, with the proviso that at least one of X and Z is an alkenyl equivalent to said group, and polymers of this monomer. One typical instance of the monomer is benzyl 6-acrylaminopenicillanate.