The stereoselective synthesis of (1S,2S,5R)-5-((4-methoxybenzyl)oxy)-2-methyl-8-methylene-1,2,4a,5,6,7,8,8a-octahy-dronaphthalene-1-carboxylic acid (2) is described, which comprises the bicyclic core structure natural product amycolamicin (1). ring-system was established via an intramolecular Diels-Alder reaction a triene carrying SuperQuat chiral auxiliary. latter could be readily removed by m...

A facile synthetic route of rivaroxaban has been developed. Using commercially available (R)-epichlorohydrin and bromobenzene as the starting materials, rivaroxaban was obtained in 39% overall yield using a Goldberg coupling as the key step. The synthetic route represents a convenient procedure for the production of rivaroxaban.

Tedizolid phosphate is the second commercially available oxazolidinone antibiotic, although the first one in class that is dosed once daily. It is a prodrug that is rapidly converted to the active compound tedizolid. Tedizolid has activity against a wide range of gram-positive pathogens, including methicillin-resistant Staphylococcus aureus. It is approved to treat acute bacterial skin and skin...

Oxazolidinones are promising candidates for the treatment of Mycobacterium tuberculosis infections. We isolated linezolid-resistant strains from H37Rv (Euro-American) and HN878 (East-Asian) strains; resistance frequencies were similar in the two strains. Mutations were identified in ribosomal protein L3 (RplC) and the 23S rRNA (rrl). All mutant strains were cross resistant to sutezolid; a subse...

Objective To evaluate contezolid (MRX-I) antibacterial activity against Mycobacterium abscessus in vitro and vivo to assess whether MRX-I treatment can prolong survival of infected zebrafish. Methods inhibitory M. was assessed by injecting into zebrafish with green fluorescent protein-labelled . Thereafter, were treated azithromycin (AZM), linezolid (LZD) or then maximum tolerated concentration...

A series of new conjugated copolymers incorporating the redox-active pyrrolo-TTF unit has been synthesised. The properties of the polymers have been investigated by cyclic voltammetry and electronic absorption spectroscopy, revealing that the pyrrolo-TTF behaves very differently to its thieno-TTF variant. In comparison to thieno analogues, the band gaps of the new polymers are wider than expect...

Prolonged treatment with the oxazolidinone linezolid is associated with myelosuppression, lactic acidosis, and neuropathies, toxicities likely caused by impairment of mitochondrial protein synthesis (MPS). To evaluate the potential of the novel oxazolidinone tedizolid to cause similar side effects, nonclinical and pharmacokinetic assessments were conducted. In isolated rat heart mitochondria, t...

Thrombocytopenia is a common side effect of linezolid, an oxazolidinone antibiotic often used to treat multidrug-resistant Gram-positive bacterial infections. Various risk factors have been suggested, including linezolid dose and duration of therapy, baseline platelet counts, and renal dysfunction; still, the mechanisms behind this potentially treatment-limiting toxicity are largely unknown. A ...