Developing a highly validated and sensitive HPLC method for simultaneous estimation of cefotaxime and paracetamol in pure and pharmaceutical preparations

An isocratic HPLC technique was exploited and validated for the quick simultaneous separation and measurement of cefotaxime and paracetamol in vials dosage forms, with a total analysis time of 3 minutes. The process of separation was carried out on a Thermo Scientific® Venusil XBPC18 (L) (5µm, 4.6x250 mm) using a mobile phase of ACN: distilled water (70:30, v/v) at the ambient temperature. The flow rate used in the experiment was 1 mL/min, and the highest level of absorption was determined by high-performance liquid chromatography with photodiode array detection (HPLC-PDA) employing a PDA detector set at a wavelength of 255 nm. The established retention times for cefotaxime and paracetamol were 1.79 and 2.97 minutes, respectively, suggesting reduced analysis duration. The observed limits of detection for ceftaxime and paracetamol were 4.2×10-5 and 1.2×10-5 µg/mL, respectively, indicating a significant level of sensitivity in the approach. The approach was subsequently verified in accordance with the requirements set out by the Food and Drug Administration (FDA) for the quantification of medicines in vial dosage form

Targeting methionyl tRNA synthetase: design, synthesis and antibacterial activity against Clostridium difficileof novel 3-biaryl-N-benzylpropan-1-amine derivatives

The synthesis of a series of benzimidazole-N-benzylpropan-1-amines and adenine-N-benzylpropan-1-amines is described. Subsequent evaluation against two strains of the anaerobic bacterium Clostridium difficile was performed with three amine derivatives displaying MIC values of 16 μg/mL. Molecular docking studies of the described amines determined that the amines interact within two active site pockets of C. difficile methionyl tRNA synthetase with methoxy substituents in the benzyl ring and an adenine biaryl moiety resulting in optimal binding interaction

Colistin Sulfate Chiral Stationary Phase for the Enantioselective Separation of Pharmaceuticals Using Organic Polymer Monolithic Capillary Chromatography

A new functionalized polymer monolithic capillary with a macrocyclic antibiotic, namely colistin sulfate, as chiral selector was prepared via the copolymerization of binary monomer mixtures consisting of glycidyl methacrylate (GMA) and ethylene glycol dimethacrylate (EGDMA) in porogenic solvents namely 1-propanol and 1,4-butanediol, in the presence of azobisiso-butyronitrile (AIBN) as initiator and colistin sulfate. The prepared capillaries were investigated for the enantioselective nano-LC separation of a group of racemic pharmaceuticals, namely, α- and β-blockers, anti-inflammatory drugs, antifungal drugs, norepinephrine-dopamine reuptake inhibitors, catecholamines, sedative hypnotics, antihistaminics, anticancer drugs, and antiarrhythmic drugs. Acceptable separation was achieved for many drugs using reversed phase chromatographic conditions with no separation achieved under normal phase conditions. Colistin sulfate appears to be useful addition to the available macrocyclic antibiotic chiral phases used in liquid chromatography

Daptomycin: A Novel Macrocyclic Antibiotic as a Chiral Selector in an Organic Polymer Monolithic Capillary for the Enantioselective Analysis of a Set of Pharmaceuticals:A novel macrocyclic antibiotic as a chiral selector in an organic polymer monolithic capillary for the enantioselective analysis of a set of pharmaceuticals

Daptomycin, a macrocyclic antibiotic, is here used as a new chiral selector in preparation of chiral stationary phase (CSP) in a recently prepared polymer monolithic capillary. The latter is prepared using the copolymerization of the monomers glycidyl methacrylate (GMA) and ethylene glycol dimethacrylate (EGDMA) in the presence of daptomycin in water. Under reversed phase conditions (RP), the prepared capillaries were tested for the enantioselective nanoliquid chromatographic separation of fifty of the racemic drugs of different pharmacological groups, such as adrenergic blockers, H1-blockers, NSAIDs, antifungal drugs, and others. Baseline separation was attained for many drugs under RP-HPLC. Daptomycin expands the horizon of chiral selectors in HPLC

Adenine and benzimidazole-based mimics of REP-3123 as antibacterial agents against Clostridium difficile and Bacillus anthracis: Design, synthesis and biological evaluation

As part of our ongoing research efforts to develop new antibacterial agents acting on novel molecular targets, a series of twenty-two adenine and benzimidazole-based mimics of the lead compound REP-3123 was designed to target methionyl-tRNA synthetase of Clostridium difficile and Bacillus anthracis based on a homology model. Structures of the target compounds were elucidated by means of 1H and 13C NMR spectral data and their purity was confirmed by HRMS or microanalyses. The target compounds were tested for their in vitro antibacterial activity against those two challenging organisms by the microdilution method in brain heart infusion broth. Unfortunately, six of the target compounds were not biologically tested due to inadequate solubility in DMSO under the assay conditions. Only the fluoro-substituted adenine-based sulfamide (18) showed activity against C. difficile with an MIC of 85.33 μg/mL. The adenine-based thiourea (32) and diamine (36) were the most promising antibacterial agents against B. anthracis with an MIC of 92.16 μg/mL. The rest of the tested compounds either showed inferior activity (MIC = 102.4 μg/mL) or were totally inactive. Although the compounds were not very active, the biological data are employed as a basis for our currently underway investigation for structure optimization

Targeting methionyl tRNA synthetase: design, synthesis and antibacterial activity against Clostridium difficile

The synthesis of a series of benzimidazole-N-benzylpropan-1-amines and adenine-N-benzylpropan-1-amines is described. Subsequent evaluation against two strains of the anaerobic bacterium Clostridium difficile was performed with three amine derivatives displaying MIC values of 16 μg/mL. Molecular docking studies of the described amines determined that the amines interact within two active site pockets of C. difficile methionyl tRNA synthetase with methoxy substituents in the benzyl ring and an adenine biaryl moiety resulting in optimal binding interaction

Targeting methionyl tRNA synthetase: design, synthesis and antibacterial activity against <i>Clostridium difficile</i> of novel 3-biaryl-<i>N</i>-benzylpropan-1-amine derivatives

<p>The synthesis of a series of benzimidazole-<i>N</i>-benzylpropan-1-amines and adenine-<i>N</i>-benzylpropan-1-amines is described. Subsequent evaluation against two strains of the anaerobic bacterium <i>Clostridium difficile</i> was performed with three amine derivatives displaying MIC values of 16 μg/mL. Molecular docking studies of the described amines determined that the amines interact within two active site pockets of <i>C. difficile</i> methionyl tRNA synthetase with methoxy substituents in the benzyl ring and an adenine biaryl moiety resulting in optimal binding interactions.</p