ABSTRACT A new selective and sensitive high‐performance liquid chromatography (HPLC) method was developed for the quantification of potential impurities in fluoxetine hydrochloride. Chromatographic separation was achieved on an end‐capped octadecylsilyl silica gel (Gemini‐C18 150 mm × 4.6 mm, 3.0 μm) using a gradient program with triethylamine, methanol, and water as the mobile phase at a flow rate of 1.0 mL/min and monitored at 215 nm. The run time was 60 min. The method was validated to fulfill International Conference on Harmonization (ICH Q2(R2)) requirements, and this validation included specificity, precision, linearity, limit of detection (LOD), limit of quantification (LOQ), and accuracy. The calibration curve was linear over the concentration range from LOQ to 120% with respect to sample concentration. The accuracy of the method is within the acceptable limit of 80%–120%. The results obtained for all parameters were within the acceptance criteria. So, this method can be employed for the regular analysis of potential impurities in the fluoxetine hydrochloride API.
Abstract The title compounds (III) are obtained via a two‐step one‐pot synthesis involving the construction of the cyclohexanone ring from aromatic aldehydes and β‐ketoesters as initial step under mild reaction conditions.
Compounds with a pyrrolidine scaffold play an important role in organic synthesis and especially in the synthesis of bioactive organic compounds, therefore, the development of new methods for modifying this scaffold is a very interesting framework of this study. We developed a rational approach for the synthesis of 1,2,3-trazolylchalcone substituted pyrrolidines derivatives, which were then examined using a variety of spectroscopic techniques such as 1H NMR, 13C NMR, FT-IR, mass spectroscopy and elemental analysis. Biological profiles showed that compounds 5e, 5h had better antibacterial inhibitory potency against S. aureus, E. coli with zone of inhibition 34 ± 0.1, 33 ± 0.3 mm, whereas 5a, 5e showed potent antifungal activity against C. parapsilosis, A. flavus with dimeter zone of inhibition 26 ± 0.2, and 30 ± 0.2 mm respectively. Among the tested compounds 5b, and 5h were the most potent antitubercular activity against Mycobacterium tuberculosis H37Rv and showing MIC values 5.23 µg/mL, 6.85 µg/mL respectively, which are similar activity that of the standard Streptomycin (MIC = 5.02 µg/mL). The binding mode for compound 5 inside the catalytic pocket of M. tuberculosis cytochrome P450 CYP121A1 and produced a network of hydrophobic and hydrophilic interactions (6GEO). From docking results, 5b demonstrated highly stable binding amino acids SerA:237, ArgA:386, ArgA:286, CysA:345, MetA:62, GlnA:385, AspA:282, PheA:280, LeuA:284, ValA:83, ProA:285, AlaA:337, HisA:343, AsnA:74, and ThrA:65, which are plays a crucial role in ensuring efficient binding of the ligand in a crystal structure of tubercular receptor. Furthermore, the physicochemical and ADME (absorption, distribution, metabolism, and excretion) filtration molecular properties, estimation of toxicity, and bioactivity scores of these scaffolds were evaluated.
Abstract A simple and inexpensive synthesis of novel 2-(3-oxo-3-arylpropyl)-2,3-dihydro-1H-inden-1-one derivatives has been achieved via Pd/C-mediated arylation followed by I2-mediated regioselective hydration of 2-(prop-2-ynyl)-2,3-dihydro-1H-inden-1-ones. A wide variety of 3-aryl substituted 2-propynyl indanone derivatives were conveniently prepared by using 10% Pd/C-PPh3-CuI as a catalyst system, some of which were used to prepare the corresponding ketones via alkyne hydration in the presence of catalytic I2. In an in vitro study a representative compound showed inhibition of PDE4B (phosphodiesterase type 4B) and binding with this protein in silico
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.
When it comes to solving global issues like resource conservation and ecological sustainability, chemistry is the important factor . Traditional methods of chemical synthesis frequently employ dangerous chemicals, produce large amounts of waste, and use a lot of energy, all of which contribute to pollution and the depletion of natural resources. The idea of sustainable chemistry has arisen as a guiding principle in response to these worries, seeking to design and develop chemical processes that maximize efficiency while minimizing environmental effect. (1)
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