摘要:
.beta.-Lactams having a substituted hydroxymethylene group at the position .alpha. to the lactam carbonyl group are prepared by reaction of an .alpha.-halo-.beta.-lactam with zinc or zinc amalgam in an anhydrous aprotic medium to produce an intermediate which in situ reacts with an appropriate aldehyde or ketone.Also described are novel penicillins and cephalosporins having useful antibacterial activity.
摘要:
.beta.-Lactams having a substituted hydroxymethylene group at the position .alpha. to the lactam carbonyl group are prepared by reaction of an .alpha.-halo-.beta.-lactam with zinc or zinc amalgam in an anhydrous aprotic medium to produce an intermediate which in situ reacts with an appropriate aldehyde or ketone.Also described are noval penicillins and cephalosporins having useful antibacterial activity.
摘要:
A compound represented by formula I ##STR1## wherein R is hydrogen, or ##STR2## wherein R.sup.1 is N-acylamino, N-alkylamino, N,N-dialkylamino, N-acyl-N-hydroxylamino, nitroso or the pharmaceutically acceptable salts thereof.
摘要:
3-O-Glycosyl derivatives of 16-membered macrolides such as O-.alpha.-L-cladinosyl-(1.fwdarw.3)-12,13-dehydro-12,13-deoxorosaramicin, 2", 4",4'"-tri-O-acetyl-O-(4'-O-phenoxyacetyl-.alpha.-L-cladinosyl)-(1.fwdarw.3)-desmyconsin and pharmaceutically acceptable acid addition salts thereof useful as antibacterials are disclosed.
摘要:
Everninomicin B, C or D may be converted to amino derivatives by reductive means. The amino derivatives may, subsequently, be converted to novel N-acyl, N-alkyl or N,N-dialkyl derivatives. Alternatively, everninomicins B, C or D may be converted to N-acyl-N-hydroxylamino derivatives also by reductive means. The derivatives so-produced and the non-toxic pharmaceutically acceptable cationic salts thereof are novel and are antibacterial agents.
摘要:
There is disclosed desevernitrose, acetamido, ethylamino and diethylamino derivatives of antibiotic 13-384 components 1 and 5 represented by the following formula ##STR1## wherein R is hydrogen, or ##STR2## wherein R.sup.1 is acetamide, ethylamine, diethylamine, N-hydroxylamino, nitroso or the pharmaceutically acceptable salts thereof.
摘要:
Described is a novel process for the preparation of 12,13-desepoxy-12,13-dehydrorosamicin by reducing rosamicin in a mineral acid solution containing Cr.sup.+.sup.+ cations. Rosamicin is an antibiotic elaborated by Micromonospora rosaria.
摘要:
Desmycinosyl derivatives of 12,13-desepoxy-12,13-dehydro antibiotic AR-5 component 1 and 12,13-desepoxy-12,13-dehydro antibiotic AR-5 component 2 are useful antibacterial agents and may be converted to other such agents by processes analogous to those generally known in the art.
摘要:
Novel macrolide antibacterial derivatives of the components of the Antibiotic AR-5-complex are disclosed herein. The invention specifically relates to compounds wherein the macrolide ring and/or the two attached sugars are derivatized. Also disclosed are methods for the preparation of the derivatives and methods for the use thereof.
摘要:
Everninomicin antibiotics having a nitro function, e.g. everninomicin B, everninomicin C, and everninomicin D, upon treatment with aluminum amalgam in aqueous alkanol are converted to a mixture of at least two reduction products having antibacterial activity, said reduction products being an everninomicin having a nitroso function and an everninomicin having a hydroxylamino function. The nitrosoeverninomicins are also prepared by treating the corresponding hydroxylaminoeverninomicin with an oxidizing reagent selected from the group consisting of aerial oxidation in alkaline solution, and an alkali metal hypobromite in an aprotic solvent. The everninomicin reduction products and salts thereof are described as well as nitrone derivatives of the hydroxylaminoeverninomicins and salts thereof, all of which possess antibacterial activity. A preferred compound is hydroxylaminoeverninomicin D, particularly the sodium salt thereof.