Synthesis and Pharmacological Activities of Chalcone and Its Derivatives Bearing N-Heterocyclic Scaffolds: A Review.

The incorporation of heterocyclic moieties into the standard chemical structure with a biologically active scaffold has become of crucial practice for the construction of pharmacologically potent candidates in the drug arena. Currently, numerous kinds of chalcones and their derivatives have been synthesized using the incorporation of heterocyclic scaffolds, especially chalcones bearing heterocyclic moieties that display improved efficiency and potential for drug production in pharmaceutical sectors. The current Review focuses on recent advances in the synthetic approaches and pharmacological activities such as antibacterial, antifungal, antitubercular, antioxidant, antimalarial, anticancer, anti-inflammatory, antigiardial, and antifilarial activities of chalcone derivatives incorporating N-heterocyclic moieties at either the A-ring or B-ring.

Recent advances in the synthesis of pharmaceutically active 4-quinolone and its analogues: a review.

4-Quinolone and its analogs are heterocyclic classes of organic compounds displaying biologically active and a broad spectrum of pharmaceutical drug scaffolds. 4-Quinolone is the first-line chemotherapeutic treatment for a wide spectrum of bacterial infections. Recently, 4-quinolone and its derivatives have been shown to have the potential to cure and regulate various acute and chronic diseases, including pain, ischemia, immunomodulation, inflammation, malarial, bacterial infection, fungal infection, HIV, and cancer, based on several reports. This review highlights and provides brief information to better understand the development of experimental progress made to date in the synthetic protocol towards 4-quinolone and its analogs. Thus, classical synthesis protocol, metal-free reaction protocol, and transition metal-catalyzed reaction procedures are briefly discussed along with the pharmaceutical activities of selected 4-quinolone derivatives.

Synthesis and pharmacological activities of azo dye derivatives incorporating heterocyclic scaffolds: a review.

Nowadays, there is significant interest in the synthesis of heterocycle-incorporated azo dye derivatives as potential scaffolds in the pharmaceutical sector. The pharmaceutical or drug industries need a simplistic synthesis approach that can afford a wide range of azo dye derivatives. The incorporation of the heterocyclic moiety into the azo dye scaffold has improved the bioactive properties of the target derivatives. The various biological and pharmacological applications of drugs such as anti-fungal, anti-tuberculosis, anti-viral, anti-inflammatory, anti-cancer, anti-bacterial, DNA binding, and analgesic properties can be easily tuned by introducing heterocyclic moieties. To date, continuous efforts are being made in the search for more potent, new, and safe synthetic methodologies for azo dye derivatives. This review presents a brief discussion of the facile synthetic approaches and the relevance of the title compound and its derivatives towards various biological activities. Thus, the synthesis of azo dye derivatives incorporating heterocyclic scaffolds such as imidazole, pyrazole, thiazole, oxazolone, thiophene, pyrrole, benzothiazole and quinoline moieties and their pharmacological applications are discussed briefly.

Biogenic Synthesis of Cu-Doped ZnO Photocatalyst for the Removal of Organic Dye.

The Cu-doped ZnO photocatalysts were prepared with a green and coprecipitation approach by using water hyacinth (Eichhornia crassipes) aquatic plant extract. In the preparation process, different amount of copper precursors such as 1, 2, 3, 4, and 5% of molar ratio were added to zinc nitrate precursors and abbreviated as Cu-ZnO (1%), Cu-ZnO (2%), Cu-ZnO (3%), Cu-ZnO (4%), and Cu-ZnO (5%), respectively. The characterization of the obtained samples was carried out, and the removal of the methylene blue (MB) dye was examined. Out of all catalysts, Cu-ZnO (3%) had the best photocatalytic performance and 89% of the MB dye was degraded. However, the degradation performances of blank (without catalysts), ZnO, Cu-ZnO (1%), Cu-ZnO (2%), Cu-ZnO (4%), and Cu-ZnO (5%) catalysts were 6, 54, 69, 83, 80, and 73%, respectively. Therefore, the use of water hyacinth plant extract with the optimum amount of Cu added to ZnO during the preparation of the catalyst could have a promising application in the degradation of organic pollutants.

Synthesis of Benzimidazole-Sulfonyl Derivatives and Their Biological Activities.

Currently, the synthesis of new compounds with potential bioactivities has become a central issue in the drug discovery arena. Among these new compounds, benzimidazole-sulfonyl scaffolds have vital applications in the fields of pharmaceuticals industries. Benzimidazole and sulfonyl compounds have remarkable biological activities, such as antibacterial, antifungal, anti-inflammatory, antiproliferative, carbonic anhydrase inhibitory, and α-amylase inhibitory activities. Furthermore, recent literature mentions the synthesis and bioactivities of some benzimidazole-sulfonyl hybrids. In this review, we focus on reviewing the synthesis of these hybrid scaffolds and their various types of biological activities of the compounds.

Antibacterial, Docking, DFT and ADMET Properties Evaluation of Chalcone-Sulfonamide Derivatives Prepared Using ZnO Nanoparticle Catalysis.

INTRODUCTION: In the present work, two novel compounds were synthesized using zinc oxide nanoparticles through green synthesis protocol. The zinc oxide nanoparticles catalyzed reactions were afforded good to excellent yields of the target compounds 76.3-98.6%. METHODOLOGY: The synthesized compounds were characterized by UV-Vis, IR and NMR. The antibacterial activity of the synthesized compounds was screened against two Gram-positive bacteria (Bacillus cereus and Staphylococcus aureus) and two Gram-negative bacteria (Escherichia coli and Salmonella typhimurium). RESULTS AND DISCUSSION: The synthesized compounds displayed potent activity against the bacterial strains. Among them, compound 8 showed strong activity against Bacillus cereus relative to the standard drug. On the other hand, compound 9 exhibited strong activity against Escherichia coli. The molecular docking study of the synthesized compounds was conducted to investigate their binding pattern with DNA gyrase and E. coli dihydropteroate synthase and all of them were found to have minimum binding energy ranging from -6.0 to -7.3 kcal/mol, and the best result achieved with compound 8 and 9. CONCLUSION: The findings of the in vitro antibacterial and molecular docking analysis demonstrated that the synthesized compounds have potential of antibacterial activity and can be further optimized to serve as a lead compound.

Synthesis, DFT Analysis, and Evaluation of Antibacterial and Antioxidant Activities of Sulfathiazole Derivatives Combined with In Silico Molecular Docking and ADMET Predictions.

Synthetic modifications of sulfathiazole derivatives become an interesting approach to enhance their biological properties in line with their applications. As a result, sulfathiazole derivatives become a good candidate and potential class of organic compounds to play an important role towards medicinal chemistry. In present study, one thiazole derivative and two new sulfathiazole derivatives are synthesized with 94% and 72-81% yields, respectively. Furthermore, the synthesized compounds were evaluated for their in vitro antibacterial activity against two Gram-negative (E. coli and P. aeruginosa) and two Gram-positive bacterial strains (S. pyogenes and S. aureus) by disk diffusion method. Among synthesized compounds, compound 11a showed potent inhibitory activity against Gram-negative, E. coli with 11.6 ± 0.283 mm zone of inhibition compared to standard drug sulfamethoxazole (15.7 ± 0.707 mm) at 50 mg/mL. The radical scavenging activities of these compounds were evaluated using DPPH radical assay, and compound 11a showed the strongest activity with IC50 values of 1.655 µg/mL. The synthesized compounds were evaluated for their in silico molecular docking analysis using S. aureus gyrase (PDB ID: 2XCT) and human myeloperoxidase (PDB ID: 1DNU) and were found to have minimum binding energy ranging from -7.8 to -10.0 kcal/mol with 2XCT and -7.5 to -9.7 with 1DNU. Compound 11a showed very good binding score -9.7 kcal/mol with both of the proteins and had promising alignment with in vitro results. Compound 11b also showed high binding scores with both proteins. Drug likeness and ADMET of synthesized compounds were predicted. The DFT analysis of synthesized compounds was performed using Gaussian 09 and visualized through Gauss view 6.0. The structural coordinates of the lead compounds were optimized using B3LYP/6-31 G (d,p) level basis set without any symmetrical constraints. Studies revealed that all the synthesized compounds might be candidates for further antibacterial and antioxidant studies.

Recent advances in the synthesis of biologically and pharmaceutically active quinoline and its analogues: a review.

Recently, quinoline has become an essential heterocyclic compound due to its versatile applications in the fields of industrial and synthetic organic chemistry. It is a vital scaffold for leads in drug discovery and plays a major role in the field of medicinal chemistry. Nowadays there are plenty of articles reporting syntheses of the main scaffold and its functionalization for biological and pharmaceutical activities. So far, a wide range of synthesis protocols have been reported in the literature for the construction of this scaffold. For example, Gould-Jacob, Friedländer, Pfitzinger, Skraup, Doebner-von Miller and Conrad-Limpach are well-known classical synthesis protocols used up to now for the construction of the principal quinoline scaffold. Transition metal catalysed reactions, metal-free ionic liquid mediated reactions, ultrasound irradiation reactions and green reaction protocols are also useful for the construction and functionalization of this compound. The main part of this review focuses on and highlights the above-mentioned synthesis procedures and findings to tackle the drawbacks of the syntheses and side effects on the environment. Furthermore, various selected quinolines and derivatives with potential biological and pharmaceutical activities will be presented.