RP-LC Analysis and Hydrolytic Degradation Profile of Racecadotril

A sensitive, stability-indicating liquid-chromatographic method for analysis of racecadotril in the presence of its degradation products has been developed and validated. Efficient chromatographic separation was achieved on a C₁₈ column with a simple isocratic mobile phase—60:40 methanol–water. Quantification was by photo-diode array (PDA) detection at 220 nm. The linearity of the method was excellent over the range 1–32 μg mL^?1. The method was sensitive, with low limits of detection (20 ng mL^?1) and quantification (100 ng mL^?1). The recovery of the method was consistently good (98.7–100.9%), with low (<1%) intra-day and inter-day relative standard deviation. Robustness studies confirmed that peak area was unaffected by small changes in temperature, and mobile phase composition and flow rate. Both alkaline and acidic hydrolytic degradation were performed in methanolic solution. In alkaline medium the drug was degraded immediately; it was degraded within 90 min in acidic medium. The validated, stability-indicating, method was used for analysis of racecadotril in pharmaceutical dosage form and also to reveal the hydrolytic degradation profile of the racecadotril.     

Highly regioselective ring opening of oxiranes with phenoxides in the presence of beta-cyclodextrin in water

Highly regioselective ring opening of oxiranes to beta-hydroxy ethers with phenoxides has been achieved in impressive yields in the presence of beta-cyclodextrin as catalyst and water as solvent.     

Highly selective oxidative cleavage of beta-cyclodextrin-epoxide/aziridine complexes with IBX in water

Water, an environmentally friendly reaction medium, has been utilized for the reaction of IBX with various epoxides 1 and aziridines 2 as their beta-cyclodextrin complexes to afford for the first time alpha-hydroxyketones 3 and alpha-aminoketones 4, respectively.     

Design,Synthesis, and Biological Evaluation of 3,5‐Disubstituted 2‐Pyrazineamide Derivatives as Antitubercular Agents

A novel series of 3,5‐disubstituted‐2‐pyrazineamide derivatives ( 5a–5o ) were synthesized and studied for their potential as antitubercular agents. Among them, the compounds 5a , 5g , and 5m showed the good minimal inhibitory concentration of 20, 25, and 25 μg/mL, respectively. The compound 5a displayed excellent minimum inhibitory concentration of 10 μg/mL and is four times more potent compared with the standard drug, rifampicin concentration. In silico docking studies revealed that the compounds 5a and 5c can bind strongly in the active site of 2FUM enzyme and prevent enzyme–substrate interactions. In addition, in silico docking studies were calculated, and based on the data obtained, compound 5a displayed excellent drug‐like properties.     

Refining comparative proteomics by spectral counting to account for shared peptides and multiple search engines

Spectral counting has become a widely used approach for measuring and comparing protein abundance in label-free shotgun proteomics. However, when analyzing complex samples, the ambiguity of matching between peptides and proteins greatly affects the assessment of peptide and protein inventories, differentiation, and quantification. Meanwhile, the configuration of database searching algorithms that assign peptides to MS/MS spectra may produce different results in comparative proteomic analysis. Here, we present three strategies to improve comparative proteomics through spectral counting. We show that comparing spectral counts for peptide groups rather than for protein groups forestalls problems introduced by shared peptides. We demonstrate the advantage and flexibility of this new method in two datasets. We present four models to combine four popular search engines that lead to significant gains in spectral counting differentiation. Among these models, we demonstrate a powerful vote counting model that scales well for multiple search engines. We also show that semi-tryptic searching outperforms tryptic searching for comparative proteomics. Overall, these techniques considerably improve protein differentiation on the basis of spectral count tables.     

Reagent‐Based DOS: Developing a Diastereoselective Methodology to Access Spirocyclic‐ and Fused Heterocyclic Ring Systems

Herein, we report a diversity‐oriented‐synthesis (DOS) approach for the synthesis of biologically relevant molecular scaffolds. Our methodology enables the facile synthesis of fused N‐heterocycles, spirooxoindolones, tetrahydroquinolines, and fused N‐heterocycles. The two‐step sequence starts with a chiral‐bicyclic‐lactam‐directed enolate‐addition/substitution step. This step is followed by a ring‐closure onto the built‐in scaffold electrophile, thereby leading to stereoselective carbocycle‐ and spirocycle‐formation. We used in silico tools to calibrate our compounds with respect to chemical diversity and selected drug‐like properties. We evaluated the biological significance of our scaffolds by screening them in two cancer cell‐lines. In summary, our DOS methodology affords new, diverse scaffolds, thereby resulting in compounds that may have significance in medicinal chemistry.     

Structural, optical and thermal investigations on Dy doped NaF–Li2O–B2O3 glasses

Structural, optical and thermal properties of Dy³⁺ doped lithium fluoroborate glasses have been studied for various concentrations of Dy³⁺ from 0.5 to 5 wt%. The XRD studies confirm the amorphous nature of the glasses while the FTIR spectra reveal the presence of BO₃ and BO₄ local structural units. The UV–VIS–NIR absorption studies were carried out to calculate the bonding parameters ( and δ), to identify the ionic/covalent nature of the glasses. The JO parameters, experimental and theoretical oscillator strengths were also determined and reported. The luminescence spectra have been studied to determine the radiative transition probability (A), stimulated emission cross section () and the experimental and calculated branching ratios (β_R) for the excited levels that include ⁴F_9/2→⁶H_11/2, ⁶H_13/2, and ⁶H_15/2 transitions. The variation of optical properties with varying concentrations of dysprosium oxide content in the glasses are reported and discussed. The thermal behavior of Dy³⁺ doped lithium fluoroborate glasses have been reported by recording DSC thermograms.     

A multi-criteria decision making model for advanced repair-to-order and disassembly-to-order system

Sensor-embedded products (SEPs) eliminate a majority of uncertainties involved in product recovery by providing item-based life-cycle information. This information includes the content of each product and component conditions, and enables the estimation of remaining useful life of the components. Once the data on the products are captured, it is possible to make optimal recovery decisions without any preliminary disassembly or inspection operations.