Abstract: It is an object of the present invention to provide antimicrobial metallodrugs comprising an antimicrobial peptide (“AMP”) and/or an antibiotic covalently bound to a metal binding moiety. These metallodrugs combine a metal binding domain which typically catalyzes oxido-reductase chemistry or acts as a Lewis-Acid catalyst, with a member of a diverse class of antimicrobial agents currently validated in preclinical and clinical settings for the treatment of a broad spectrum of pathogenic organisms.

Abstract: It is an object of the present invention to provide antimicrobial metallodrugs comprising an antimicrobial peptide (“AMP”) and/or an antibiotic covalently bound to a metal binding moiety. These metallodrugs combine a metal binding domain which typically catalyzes oxido-reductase chemistry or acts as a Lewis-Acid catalyst, with a member of a diverse class of antimicrobial agents currently validated in preclinical and clinical settings for the treatment of a broad spectrum of pathogenic organisms.

Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of antimicrobials and antimicrobial-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

Abstract: The present invention refers to the preparation process of the sodium salt of 6[D-(−)&agr;-4-(ethyl-2,3-dioxo-1-piperazinocarbonylamino) phenylacetamido]penicillanic acid, comprising the reaction of the acid with a reagent selected from the group consisting of sodium hydroxide, sodium carboxylates and sodium alcoholates, followed by a separation step of the so obtained sodium salt by precipitation.

Abstract: A process for producing a compound of the formula ##STR1## comprises the following sequence of steps: ##STR2## wherein the various radicals are as defined in the specification.

Abstract: The 6-[D(-)-alpha(4-ethyl-2,3-dioxopiperazin-1-ylcarbonylamino)-alphaphenylace tamido]penicillanic acid and the salts thereof are prepared by synthetizing the novel intermediates, thioesters of D(-)-alpha-(4-ethyl-2,3-dioxopiperazin-1-ylcarbonylamino)-alpha-phenylacet ic acid, with mercaptoheterocycles and by converting them into the desired compound by reaction with 6-amino-penicillanic acid.

Abstract: Improved process for the preparation of 6-substituted penicillanic acids, in particular 6[D(-)-.alpha.-(4-alkyl-2,3-dioxo-]-piperazinocarbonylamino)phenylacetamid o]penicillanic acids, and the pharmaceutically acceptable salts thereof.

Abstract: .beta.-Lactam antibiotics having an .alpha.-formamido substituent on the carbon atom adjacent to the carbonyl group of the .beta.-lactam ring and in particular bicyclic compounds having the partial structure: ##STR1## Intermediates and processes for the preparation of the compounds are further disclosed.