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Increased use of antibiotics globally has led to the threat of antibiotic resistance; this drove the urge of researchers toward discovering more potent and broad-spectrum antibiotics. Levonadifloxacin (LND) is the very first antibiotic developed by an Indian company Wockhardt. It is S (–) isomer of another broad-spectrum antibiotic Nadifloxacin which is used topically for skin, soft tissue bacterial infection. LND belongs to the benzo quinolizine category which is a subclass of fluoroquinolone, indicated for ABSSIS, CABP, and other infections including diabetic foot infection; formulated as l-arginine salt of levonadifloxacin (WCK177) for IV and l-alanine ester mesylate salt as alalevonadifloxacin (WCK2349) for oral administration. It generally shows dominant antibacterial activity against Gram-negative, and positive bacterial infections, particularly toward methicillin-resistant Staphylococcus aureus (MRSA) by dual inhibition of DNA gyrase and topoisomerase IV. Producing quality product that complies to regulatory requirements is a big concern for pharma industries. To this context, validated analytical methods for routine quality control are essential for quantification of LND as an API alone and together with pharmaceutical formulations. This review suggests therapeutic, pharmacological, and analytical aspects regarding the novel drug LND and particularly focuses on discussing various reported analytical methods present for analytical or bioanalytical estimation of the drug and suggest to develop a simple and validated method which also complies to green chemistry. [ABSTRACT FROM AUTHOR]

Monoterpene derivatives are of great biological relevance in the pharmaceutical industry. In the present study, pyrrolidine derivative of a carvotacetone, 3-O-benzylcarvotacetone (1), and selected monoterpenes (3-hydroxy-2-isopropyl-5-methyl-p-benzoquinone (3) and cis-piperitol (5)) were prepared to provide (R)-1-(4-(benzyloxy)-5-isopropyl-2-methylcyclohexa-1,3-dien-1-yl)-pyrrolidine (2), 2-isopropyl-5-methyl-3,6-dioxocyclohexa-1,4-dien-1-yl acetate (4), cis-3-hydroxypiperitone (6) and carvacrol (7). Structure of 2 was determined based on NMR and HRMS spectral data. Compound 4 exhibited activity against fungi Cryptococcus neoformans with an IC50 value of < 0.8 µg/mL. In addition, this compound 4 had an IC50 value of 14.97 µg/mL against methicillin resistant Staphylococcus aureus bacteria. Previous to the current study, both compound 6 and 7 had been reported to have anti-microbial and anti-fungal activities. [ABSTRACT FROM AUTHOR]

This work reports for the first time the anti-MRSA activity of the essential oil and ethanol extract ofLavandula multifidaL. on clinical and reference strains of methicillin-resistantStaphylococcus aureus(MRSA). Hospitalized patients with infected wounds at the University Hospital of Tlemcen constitute the source of collection for different clinical isolates used in this study. The oils of fresh samples were obtained by hydrodistillation at three developmental stages (before inflorescence, full-inflorescence and afterinflorescence). The oils from the aerial parts ofL. multifidawere analyzed at three developmental stages. Oil yield was found to vary depending on the stage of development and the highest content of oil (0.2% w/w) was obtained at full-inflorescence. The chemical composition of essential oils studied by GC and GC-MS showed that the main components were carvacrol (from 27.5 to 57%), β-bisabolene (from 25.2 to 38.4%) and caryophyllene oxide (from 3.5 to 7.5%). The Anti-MRSA activity ofL. multifidaessential oil and ethanol extract was tested by using disc diffusion method and microtiter plates perform for determining their minimum inhibitory concentration (MIC) values. We found a good anti-MRSA activity ofL. multifidaessential oil since the inhibition diameters reached 27 mm and MICs were lower than 0.1 μl/ml, whereas the ethanol extract was less active. These results seem to be interesting for applications ofL. multifidaessential oil to fight against MRSA. [ABSTRACT FROM PUBLISHER]

A new drimane sesquiterpenoid glycoside, named 7-drimen-3β,11-diol 3-O-β-d-glucopyranoside, was isolated from the 95% EtOH extract of the seeds of Antiaris toxicaria (Pers.) Lesch. The chemical structure was completely elucidated using a combination of 1D and 2D NMR techniques (COSY, HMQC, HMBC, and ROESY) and HR-ESI-MS analysis. The compound showed inhibitory activities toward methicillin-resistant Staphylococcus aureus (MRSA), chronic myelogenous leukemia (K562), and human hepatoma (SMMC-7721) cell lines. [ABSTRACT FROM AUTHOR]