Antibacterial/antibiotic drugs have tremendously improved the health of humans and animals since the antibiotic golden age up to date. Currently the emergence of antibiotic/antibacterial resistance due to irrational drug use in medical and veterinary practice, food industries, agriculture and in communities is posing a global health problem. Most of the unused drugs, drug metabolites and residu...

OBJECTIVES Mycobacterium avium subspecies paratuberculosis (MAP) has been targeted for treatment with clarithromycin and rifamycin derivatives in numerous cases of Crohn's disease (CD). 6-Mercaptopurine and its pro-drug azathioprine are widely used as immunomodulators in the treatment of CD and have recently been shown to have anti-MAP activity in vitro. The objectives of the study were to eval...

34 Emergence of drug-resistant bacteria represents a high, unmet medical need and discovery of 35 new antibacterials acting on new bacterial targets is strongly needed. ATP synthase has been 36 validated as antibacterial target in Mycobacterium tuberculosis, where its activity can be 37 specifically blocked by the diarylquinoline TMC207. However, potency of TMC207 is 38 restricted to mycobacter...

NCS mice gained weight rapidly when fed a gluten diet deficient in several amino acids, but their weight gain on the same regimen was very much retarded if they were given antibacterial drugs, even for a short period of time. This retardation of growth could not be entirely corrected by supplementing the gluten diet with lysine and threonine. The decrease in growth rate brought about by antibac...

OBJECTIVES Pyrrolobenzodiazepine (PBD) dimers, tethered through inert propyldioxy or pentyldioxy linkers, possess potent bactericidal activity against a range of Gram-positive bacteria by virtue of their capacity to cross-link duplex DNA in sequence-selective fashion. Here we attempt to improve the antibacterial activity and cytotoxicity profile of PBD-containing conjugates by extension of dime...

As novel and drug-resistant bacterial strains continue to present an emerging health threat, the development of new antibacterial agents is critical. This includes making improvements to existing antibacterial scaffolds as well as identifying novel ones. The aim of this study is to apply a Bayesian classification QSAR approach to rapidly screen chemical libraries for compounds predicted to have...

The antibacterial therapeutic area has been described as the perfect storm. Resistance is increasing to the point that our hospitals encounter patients infected with untreatable pathogens, the overall industry pipeline is described as dry and most multinational pharmaceutical companies have withdrawn from the area. Major contributing factors to the declining antibacterial industry pipeline incl...

tilmicosin (tlm) is an important antibiotic in veterinary medicine with low bioavailability and safety. this study aimed to formulate and evaluate physicochemical properties, storage stability after lyophilization and antibacterial activity of three tlm-loaded lipid nanoparticles (tlm-lnps) including solid lipid nanoparticles (slns), nanostructured lipid carriers (nlcs) and lipid-core nanocapsu...

A class of innovative benzimidazole-1,3,4-Oxadiazole derivatives is a significant heterocyclic molecule for therapeutic development. In chemistry, the novel 1,3,4-Oxadiazole nucleus has wide range uses, including antibacterial, treatment. Molecular docking frequently employed in contemporary drug design to comprehend drug-receptor interaction. Swiss dock, PyRx, and discovery studio visualizer (...

background: antibiotic resistant bacteria can be considered as a main problem in infection management. zinc oxide nanoparticles (zno nps), individually or in combination with antibiotics, can be considered as good candidates for struggling against drug resistant bacteria. methods: in this study, zinc oxide nanoparticles were synthesized using sol-gel method in low temperature as a cost effectiv...