Described herein are bisphosphonate quinolone compounds, conjugates and pharmaceutical formulations thereof that can include a bisphosphonate and a quinolone, where the quinolone can be releasably coupled to the bisphosphonate. Also provided herein are methods of making and methods of using the bisphosphonate quinolone compounds, conjugates and pharmaceutical formulations thereof.

The present invention provides a use of a rifamycin-quinolizidone coupling molecule, or a stereoisomer, hydrate, deuterium-substituted form, ester, solvate, crystal form, metabolite, pharmaceutically acceptable salt or prodrug thereof in resisting nontuberculous mycobacteria. The rifamycin-quinolizidone coupling molecule has a structure shown in formula (I)

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The rifamycin-quinolizidone coupling molecule, or the stereoisomer, hydrate, deuterium, ester, solvate, crystal form, metabolite, pharmaceutically acceptable salt or prodrug thereof may effectively against nontuberculous mycobacteria, and then may be used for treating infection caused by human nontuberculous mycobacteria.

The present invention relates to conjugates of aminoglycosides and terpenoids, in particular sesquiterpenoids. Furthermore, the present invention relates to nano-assemblies formed by the inventive conjugates and to a method for producing the conjugates and/or the nano-assemblies. The present invention also relates to the inventive conjugates and nano-assemblies for use in therapy, in particular for use in the treatment of infectious diseases. Particularly preferred embodiments of the present invention relate to farnesylated aminoglycosides and nano-assemblies thereof, in which farnesol and its derivatives do not only function as carrier for the aminoglycosides but do themselves have pharmaceutical activity upon cleavage of the conjugate, in particular quorum sensing inhibitory activity.

Preparation and characterization of novel DACT forms suitable for pharmaceutical compositions in drug delivery systems for humans.

Disclosed herein is an attenuated Acinetobacter baumannii comprising an expression vector comprising a nucleic acid encoding the ABUW_1645 protein or a variant thereof. Disclosed herein are methods of treating or preventing colonization, infection, or disease by an Acinetobacter baumannii microbe, the method comprising administering a clinically effective dose of the attenuated Acinetobacter baumannii to a subject in need thereof, wherein the attenuated Acinetobacter baumannii comprises an expression vector expressing the ABUW_1645 protein or variants thereof.

The present disclosure relates to novel cleavable conjugates of antibiotics and an antibacterial cell-penetrating peptide, and methods to make and use the novel cleavable conjugates of antibiotics and an antibacterial cell-penetrating peptide.

The present disclosure relates to novel antibacterial cell-penetrating peptides and derivatives, and methods to make and use the novel antibacterial cell-penetrating peptides and derivatives. The novel antibacterial cell-penetrating peptides of the present invention with shorter linker between a pyrrolidine ring and a guanidine group provide unexpectedly higher potency against a broader scope of bacterial.

A method of inhibiting anaerobic bacteria includes administering to a patient in need thereof a rifamycin-nitroimidazole conjugate molecule shown in formula I. The rifamycin-nitroimidazole conjugate molecule shown in formula I of the present invention has broad-spectrum antibacterial activity against anaerobic bacteria, including activity against most pathogenic bacteria associated with bacterial vaginosis, in vitro antibacterial activity stronger than that of drugs against bacterial vaginosis such as metronidazole and clindamycin, and potential use in prevention and treatment of bacterial vaginosis or other related diseases caused by anaerobic bacteria.

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This disclosure provides multifunctional conjugate molecules comprising a target binding component covalently linked to one or more cannabinoids and/or one or more cannabinoid conjugate components. In some embodiments, the target binding component also is covalently linked to one or more active agent components. The disclosed conjugate molecules are designed to deliver therapeutic benefits of each component of the conjugate molecules and can be used to treat cancer and other disorders.

A construct comprising: (i) an optionally derivatized glycopeptide antibiotic; (ii) a nanoparticle; and (iii) a first linker connecting (i) and (ii) is provided. The construct may further comprise a second linker located between the first linker and (ii). The nanoparticle may be a separation nanoparticle, such as a magnetic separation nanoparticle. The glycopeptide antibiotic may be selected from the group consisting: of vancomycin; teicoplanin; oritavancin; telavancin; chloroeremomycin; and balhimycin. Also provided are related methods of producing and using the construct, such as methods of separation of bacteria from a sample by binding the bacteria to the construct.