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  • Essay / Synthesis and characterization of bioactive heterocyclic molecular hybrids

    The growing interest in new drug discovery is frequently argued because drugs do not adequately increase endurance against increasing cases of cancer in the world. Molecular hybridization is a new concept in drug design and growth based on the combination of pharmacophoric moieties of different bioactive substances to produce a new hybrid compound with improved affinity and efficacy compared to the parent drugs. Say no to plagiarism. Get a tailor-made essay on “Why violent video games should not be banned”? Get the original essay Molecular hybridization is an approach to the normal design of new ligands or prototypes based on the detection of pharmacophoric subunits in the molecular structure of two or more well-known bioactive derivatives which, thanks to the ample fusion of these subunits, lead to the design of new hybrid architectures which retain the preselected characteristics of the original models. A study of the literature revealed that the history of heterocyclic chemistry began in the 1800s, alongside the development of organic chemistry. After World War II, research in the field of heterocycles experienced a massive explosion. About half of the more than six million compounds recorded in Chemical abstract are heterocyclic. Considering the use of known model substances, we have already evaluated their physicochemical and pharmacological characteristics, toxicity and mechanism of action. The triazole moiety is an important and recurring insecticide, an agrochemical structural feature of many active biological compounds such as cytochrome enzyme inhibitors and peptide analog inhibitors. The azole class of antifungal agents is a chemical group that is either a triazole or an imidazole group attached to an asymmetric carbon atom, as their functional pharmacophore treatment for these infections. Azole type antifungal agents are fluconazole, ketoconazole and ptraconazole 1, 2, 4-triazole, voriconazole are as antiasthmatic analgesic, anticholinergic activity, antibacterial. At present, cancer has gradually become the leading cause of death in all areas and seriously endangers human health and existence for a long time. It has been reported that cancer can be caused by one of three causes, namely poor diet, genetic predisposition and environmental contaminants. Pyrimidines and their derivatives have also been considered since the last century because they also possess various pharmacological properties and a wide range of biological properties. activities against unrelated DNA and RNA, diuretic, antitumor, viruses including polio viruses, anti-HIV, cardiovascular, etc. The characteristics possessed by 1,2,3-triazoles make them pharmaceutically important molecules. They are stable to reduction and oxidation as well as hydrolysis under acidic and basic conditions, indicating their strong aromatic stabilization. 1,2,3-triazoles have a high dipole moment (around 5 D) and are able to actively contribute to hydrogen bond formation as well as dipole-dipole and π-stacking interactions, which helps them to form easily bind to biological targets and improves their solubility. . The click chemistry approach invented by Sharpless using copper(I)-catalyzed azidecyne cycloaddition (CuAAC) resulted in the production of large numbers of 1,2,3-1,4-disubstituted triazoles with very high yields. Cancer is a group of diseases inin which cells develop abnormally and multiply by uncontrolled cell division. Cancer cells are more metabolically active than normal cells. It gradually invades and destroys neighboring normal cells, forming a mass called a tumor. Not all tumors or masses are benign. Tumors are not cancers. It is localized and small and tends to grow quite slowly. It does not spread to other parts of the body and is rarely life-threatening. External and internal factors such as dietary fat intake, exposure to solvents and pesticides, exposure to ionizing radiation (causing acute effects), leukemia, thyroid cancer, breast cancer, lung cancer and others), smoking, certain viruses (HIV, HPV and hepatitis B viruses) and an unhealthy lifestyle (overweight, inadequate physical exercise, excess alcohol, lack of vegetables and fruits, supplement sugar and red meat) can cause cancer. Once the DNA is affected, there is no normal control system that prevents cell proliferation and invasion of other tissues in cancer cells. Cancer is one of the most prevalent and deadly diseases, affecting one third of the world's population. Thus, molecules containing the Triazole moiety exhibit anti-cancer activities and may be able to protect against drug resistance to some extent. Cefatizine, the antibacterial agent Tazobactum as well as the anticancer agent7. In this review, we focus on the most relevant advances recorded in click chemistry reactions and synthesis under mild physiological conditions and with high efficiency and chemoselectivity. Literature review Chalcones and their derivatives are attracting increasing attention due to their numerous pharmacological applications. They are the main precursors of flavonoid biosynthesis and exhibit various biological activities such as anticancer, anti-inflammatory, nitric oxide regulators and antihyperglycemic agents. In recent years, ionic liquids have emerged as a powerful alternative to conventional molecular organic solvents due to their special properties, such as undetectable vapor pressure, wide liquid range, and ease of recovery and reuse, which which makes it a more ecological alternative to classic molecular organic solvents. volatile organic solvents. Chalcones have a wide range of biological activities and are created to be effective as antibacterial, anti-inflammatory, antifungal and anticancer, etc. Chalcones are broadly the α, β unsaturated carbonyl compounds in which they contain a ketoethylenic group. double bonds and fully delocalized π electron structure on both benzene rings. The chemistry of chalcones has given rise to intensive scientific studies throughout the world. Particular interest was focused on the synthesis and biodynamic activities of chalcones. The name “Chalcones” was assigned by Kostanecki and Tambor. These compounds are also known as benzalacetophenone or benzylidene acetophenone. In chalcones, two aromatic rings are linked by a three-carbon aliphatic chain. Chalcone has a very good synthon, which allows the design of a variety of new heterocyclics with a good pharmaceutical profile. Different methods are available for the preparation of chalcones8. Chalcones have simple chemistry that allows a multiplicity of substitutions with easy synthesis. Currently, various methods and schemes are available for the synthesis of chalcone derivatives. In eachOf these methods, the most important part is the condensation of two aromatic systems (with nucleophilic and electrophilic groups) to give the chalcone scaffold. Despite the multiplicity of permitted substitutions, we describe below the reaction scheme using the standard chalcone (1,3-diphenyl-2-propen-1-one) scaffold. Claisen-Schmidt condensationThe Claisen-Schmidt condensation is l one of the most common. In this reaction, chalcones are formed by condensation of benzaldehyde and acetophenone derivatives in the presence of alkaline or acid catalysts in a liquid solvent at 50-100 °C for several hours. The conventional Claisen-Schmidt reaction is usually carried out in the liquid phase, but some reactions can take place in the solid phase (e.g. acetophenone derivatives are mainly bound to the resin and then treated with benzaldehyde derivatives) or in the solid phase. without solvent (for example, condensation in the presence of triazabicyclodecene catalyst). Additionally, the use of microwaves in liquid and solvent-free Claisen-Schmidt reactions reduces synthesis time and produces good quantities of chalcones8. Coupling reaction Chalcones are also synthesized by a coupling reaction between benzaldehyde and phenylacetylene in presence of HBr and ionic liquids, such as 1-butyl-3-methyl-1H-imidazolium 4-methylbenzenesulfonate for 12 h at 100 °C 9. Heck carbonylative coupling reaction In the Heck carbonylative coupling reaction, the Chalcones are synthesized by carbonylation vinylation of phenyl halide with styrene in the presence of carbon monoxide and using palladium (Pd) as catalyst. One-pot synthesis One-pot synthesis is a simple but effective green method that allows the synthesis of chalcones in a single reactor. This process offers several advantages, such as increased reaction efficiency and avoidance of the lengthy purification process of intermediate chemical compounds, thereby saving resources and time. The reaction consists of a mixture of phenylmethanol and acetophenone in the presence of the oxidizing agent CrO3. Keep in mind: this is just a sample. Get a personalized article from our expert writers now. Get a Custom Essay In this reaction, CrO3 plays the vital role of generating benzaldehyde from phenylmethanol, which further reacts with acetophenone to produce the desired chalcone. Bioactivity of triazole Nucleu. Click Chemistry of 1,2,3-Triazole 45. 1,2,3-Triazole is an important heterocycle well-known in synthetic and medicinal chemistry due to its simple synthesis via click chemistry approach and a wide range of biological activities. Simple copper-catalyzed 1,3-dipolar cycloadditions of substituted azides and alkynes afford regioselective 1,4-disubstituted 1,2,3-triazoles in high yields. 1,2,3-Triazole with high dipole moment, considerable stability and hydrogen bonding capacity make it a favorable binder for biomolecular targets. 1,2,3-triazole derivatives have been reported to exhibit various biological activities such as antidiabetic, antituberculosis, anti-inflammatory, antifungal, antiviral, and antibacterial. Several drugs such as carboxyamidotriazole, cefatrizine and tazobactam contain 1,2,3-triazole in their structure. Since Sharpless and colleagues' seminal report on the concept of "click chemistry", a large number of papers have been published on the use of this compound. The prototypical click reaction constituted the copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC) to give 1,4-disubstituted 1,2,3-triazoles in very high yields under mild conditions. This catalyzed reaction. 416.