Chromatographic Methods for the Analysis of the Antipsychotic Drug Clozapine and Its Major Metabolites: A Review.

Clozapine (CLZ), a second-generation antipsychotic, can effectively reduce schizophrenia, bipolar disorder and major depression symptoms. This review provides an overview of all reported chromatographic methods (62 references) for the quantification of CLZ and its two main metabolites, norclozapine and clozapine N-oxide in pharmaceutical formulations, biological matrices and environmental samples.

Antioxidant and Antimicrobial Potential of 1,8-Naphthyridine Based Scaffolds: Design, Synthesis and in Silico Simulation Studies within Topoisomerase II.

A series of spiro ß-Lactams (4 a-c, 7 a-c) and thiazolidinones (5 a-c, 8 a-c) possessing 1,8-naphthyridine moiety were synthesized in this study. The structure of the newly synthesized compounds has been confirmed by IR, 1H-NMR, 13C NMR, mass spectra, and elemental analysis. The synthesized compounds were tested in vitro for their antibacterial and antifungal activity against various strains. The antimicrobial data showed that most of the compounds displayed good efficacy against both bacteria and fungi. The structure-activity relationship (SAR) studies suggested that the presence of electron-withdrawing chloro (3 b, 4 b, and 5 b) and nitro groups (7 b, 8 b) at the para position of the phenyl ring improved the antimicrobial activity of the compounds. The free radical scavenging assay showed that all the synthesized compounds exhibited significant antioxidant activity on DPPH. Compounds 8 b (IC50=17.68±0.76 µg/mL) and 4 c (IC50=18.53±0.52 µg/mL) showed the highest antioxidant activity compared to ascorbic acid (IC50=15.16±0.43 µg/mL). Molecular docking studies were also conducted to support the antimicrobial and SAR results.

A selective colorimetric chemosensor for detecting Ni(II) in aqueous solutions based on 4-[{[4-(3-chlorophenyl)-1,3-thiazol-2-yl]hydrazono}methyl]phenyl 4-methyl benzene sulfonate (CTHMBS).

Among the toxic heavy metals, Ni(II) can cause a variety of side effects on human health, such as allergy, cardiovascular and kidney diseases, lung fibrosis, lung, and nasal cancer. It is therefore critical from a public health and environmental perspective to determine and monitor Ni(II) ions in drinking water, foods, and environmental samples. In this study, a novel selective chemosensor (4-[{[4-(3-Chlorophenyl)-1,3-Thiazol-2-yl]Hydrazono}Methyl]phenyl4-methylBenzene Sulfonate (CTHMBS) was developed for the colorimetric detection of Ni(II) in aqueous medium. The presence of Ni(II) led to a distinct naked-eye color change from yellow to reddish-brown in aqueous solution. To examine the binding mechanism of CTHMBS to Ni(II), UV-vis spectroscopy analysis and DFT calculations were conducted. The detection limit of CTHMBS for Ni(II) was 11.87 µM, and the sensing ability of CTHMBS for Ni(II) was successfully carried out in real water samples.

Design, Synthesis, Docking Study of Pyrazolohydrazinopyrimidin-4-one Derivatives and Their Application as Antimicrobials.

New series of pyrazoles 4a-c and pyrazolopyrimidines 5a-f had been constructed. The newly synthesized compounds were assessed for their antimicrobial activity towards E. coli and P. aeruginosa (gram -ve bacteria), B. subtilis and S. aureus (gram +ve bacteria) and A. flavus and C. albicans (representative of fungi). The pyrazolylpyrimidine-2,4-dione derivative 5b is the most active candidate against B. subtilis (MIC=60 µg/mL) and P. aeruginosa (MIC=45 µg/mL). Regarding antifungal potential, compound 5f was the most effective against A. flavus (MIC=33 µg/mL). Similarly, compound 5c displayed strong antifungal activity towards C. Albicans (MIC=36 µg/mL) in reference to amphotericin B (MIC=60 µg/mL). Finally, the novel compounds had been docked inside dihydropteroate synthase (DHPS) to suggest the binding mode of these compounds.

Synthesis of Chalcones Derivatives and Their Biological Activities: A Review.

Chalcone derivatives are considered valuable species because they possess a ketoethylenic moiety, CO-CH=CH-. Due to the presence of a reactive α,ß-unsaturated carbonyl group, chalcones and their derivatives possess a wide spectrum of antiproliferative, antifungal, antibacterial, antiviral, antileishmanial, and antimalarial pharmacological properties. Recent developments in heterocyclic chemistry have led to the synthesis of chalcone derivatives, which had been biologically investigated toward certain disease targets. The major aspect of this review is to present the most recent synthesis of chalcones bearing N, O, and/or S heterocycles, revealing their biological potential during the past decade (2010-2021). Based on a review of the literature, many chalcone-heterocycle hybrids appear to exhibit promise as future drug candidates owing to their similar or superior activities compared to those of the standards. Thus, this review may prove to be beneficial for the development and design of new potent therapeutic drugs based on previously developed strategies.

Evaluation of radiological impacts of tenorm in the Tunisian petroleum industry.

The health impacts associated with uncontrolled release of TENORM in products and wastes released in the petroleum industry are of great concern. In this study, evaluation of TENORM in the Tunisian petroleum products and wastes is presented. Fourteen products samples, twelve waste samples and three samples from the surrounding environment were collected from the Tunisian Refinery STIR site and from two onshore production oilfields. The activity concentrations of (232)Th, (226)Ra and (40)K for all samples were determined using gamma-ray spectrometry with High Purity Germanium (HPGe) detector. The activity concentrations of (224)Ra were calculated only for scale samples. The radium equivalent activity, external and internal hazard indices, absorbed doses rates in air and annual effective dose were also estimated. It was noticed that maximum value of Ra(eq) activity was found to be 398 Bq/kg in scale (w8) collected from an onshore production oilfield which exceeds the maximum Ra(eq) value of 370 Bq/kg recommended for safe use. All hazard indices indicated that scale samples (w6, w7, w8 and w11) could be a significant waste problem especially sample (w8). In this study, the radium isotopic data were used to provide an estimate of scale samples ages by the use of the (224)Ra/(228)Ra activity ratio dating method. Ages of collected scales were found to be in the range 0.91-2.4 years. In this work, radioactivity (NORM contamination) in samples collected from the refinery STIR are showed to be insignificant if compared to those from onshore oilfield production sites.