摘要:
The present invention concerns neutral sugar derivatives of pradimicins, their use as antifungal agents, methods for their preparation, and intermediates for their synthesis.
摘要:
The present invention provides pradimicin analogs which exhibit improved water solubility relative to parent compounds. These novel agents are useful in treatment of fungal infections.
摘要:
This invention relates to novel cephalosporin derivatives of the formula ##STR1## wherein R.sup.1 is hydrogen, a straight, branched, or cyclic lower alkyl group having up to six carbon atoms or a radical of the formula ##STR2## in which R.sup.3 and R.sup.4 are each independently hydrogen, methyl or ethyl, or R.sup.3 and R.sup.4, taken together with the carbon atom to which they are attached, may be a cycloalkylidene ring containing from 3 to 5 carbon atoms;R.sup.2 is a radical selected from the group consisting of ##STR3## wherein R.sup.5 is hydrogen or acetyl; R.sup.6, R.sup.7 and R.sup.8 each are independently C.sub.1-5 alkyl; n is 1 or 2; and y is 1 to 5.In another aspect, this invention relates to compounds of formula I and their nontoxic pharmaeutically acceptable salts, physiologically hydrolyzable esters or solvates.Representative compounds of this invention were selected for testing and were shown to display potent antibacterial activity.
摘要:
Certain 7-acylamido-3-(2-carboxyalkyl-2,3-dihydro-s-triazolo[4,3-b]pyridazin-3-on-6-ylthiomethyl)-3-cephem-4-carboxylic acids and their salts and easily hydrolyzed esters of the 4-carboxyl group were synthesized and found to be potent antibacterial agents which exhibited good aqueous solubility. A preferred embodiment was 7-[o-(methylaminomethyl)phenylacetamido]-3-(2-carboxyalkyl-2,3-dihydro-s-triazolo[4,3-b]pyridazin-3-on-6-ylthiomethyl)-3-cephem-4-carboxylic acid.
摘要:
Certain cephalosporins having a heterocyclicthiomethyl group at the 3-position such as cefoperazone are prepared by reacting a solution of a 7-acylamidocephalosporanic acid having a free amino group as part of said acyl substituent with about an equi-molar amount of the thiolester ##STR1## wherein --S-Het is the desired conventional heterocyclicthio group which displaces the 3-acetoxy group of the starting acid and ##STR2## is the conventional acyl group which displaces a hydrogen on the free amino group which is part of the acyl substituent of the starting 7-acylamidocephalosporanic acid.
摘要:
Cephalosporins in a series having the formula ##STR1## wherein R.sup.1 is alkyl containing 1-4 carbon atoms and n is 1 or 2 or a nontoxic pharmaceutically acceptable salt thereof, were synthesized and found to be potent antibacterial agents especially when in the form of the syn isomers essentially free of the corresponding anti isomer.
摘要:
7-{(Z)-2-(2-Aminothiazol-4-yl)-2-[(substituted)oxyimino]acetamido}-3-[3-(quaternary ammonio)-1-propen-1-yl]-3-cephem-4-carboxylates and salts, esters and solvates thereof, having potent antibacterial activity, are provided. Processes for their preparation and intermediates in their preparation also are disclosed.
摘要:
Cephalosporins in a series having the formula ##STR1## wherein R.sup.1 is alkyl containing 1-4 carbon atoms or a nontoxic pharmaceutically acceptable salt thereof, were synthesized and found to be potent antibacterial agents especially when in the form of the syn isomers essentially free of the corresonding anti isomer.
摘要:
An object of the present invention is to solve problems of conventional ozone-scavenging materials and to provide an ozone-scavenging material capable of effectively decomposing/removing ozone at low cost. To attain the above object, the present invention provides an ozone-scavenging material characterized in that a metal having ozone-decomposing ability or an oxide thereof is supported on an organic polymer base having a polymer side chain having an ion exchange group on the backbone of a polymer. Said ozone-scavenging material can be prepared by introducing a polymer side chain having an ion exchange group onto the backbone of an organic polymer base, bringing the resulting organic polymer material into contact with a salt of a metal having ozone-decomposing ability to support the ion of said metal on the ion exchange group, and then precipitating fine particles of said metal or an oxide of said metal on the organic polymer material by oxidation or reduction.
摘要:
This invention provides novel cephalosporanic acids and esters thereof having the general formula ##STR1## wherein R.sup.2 is hydrogen, or lower acyl, R.sup.3 is hydrogen, or lower alkanoyloxy, andR.sup.4 is hydrogen, 5-methyl-2-oxo-1,3-dioxolen-4-ylmethyl, 1-(ethoxycarbonyloxy)ethyl,1-(pivaloyloxy)ethyl, 1-(cyclohexylacetoxy)ethyl, or 1-(cyclohexyloxycarbonyloxy) ethyl. These compounds, especially esters, are useful as broad spectrum antibiotics in the treatment and prevention of infectious diseases of mammals, and for other purposes known in the art. The acids (R.sup.4 is hydrogen) are useful as intermediates for making the esters.