Amina Benazzouz-Touami

Bio: Amina Benazzouz-Touami is an academic researcher. The author has contributed to research in topics: Chemistry & Pyrazole. The author has an hindex of 2, co-authored 4 publications receiving 14 citations.

Microwave Assisted Reactions of Azaheterocycles Formedicinal Chemistry Applications

Abstract: Microwave (MW) assisted reactions have became a powerful tool in azaheterocycles chemistry during the last decades. Five and six membered ring azaheterocycles are privileged scaffolds in modern medicinal chemistry possessing a large variety of biological activity. This review is focused on the recent relevant advances in the MW assisted reactions applied to azaheterocyclic derivatives and their medicinal chemistry applications from the last five years. The review is divided according to the main series of azaheterocycles, more precisely 5- and 6-membered ring azaheterocycles (with one, two, and more heteroatoms) and their fused analogues. In each case, the reaction pathways, the advantages of using MW, and considerations concerning biological activity of the obtained products were briefly presented.

Current Trends in Drug Delivery System of Curcumin and its Therapeutic Applications

Abstract: Curcumin is a poly phenolic compound extracted from turmeric. Over the past years, it has acquired significant interest among researchers due to its numerous pharmacological activities like anti- cancer, anti-alzheimer, anti-diabetic, anti-bacterial, anti-inflammatory and so on. However, the clinical use of curcumin is still obstructed due to tremendously poor bioavailability, rapid metabolism, lower gastrointestinal absorption, and low permeability through cell that makes its pharmacology thrilling. These issues have led to enormous surge of investigation to develop curcumin nano formulations which can overcome these restrictive causes. The scientists all across the universe are working on designing several drug delivery systems viz. liposomes, micelles, magnetic nano carriers, etc. for curcumin and its composites which not only improve its physiochemical properties but also enhanced its therapeutic applications. The review aims to systematically examine the treasure of information about the medicinal use of curcumin. This article delivers a general idea of the current study piloted to overwhelm the complications with the bioavailability of curcumin which have exhibited an enhanced biological activity than curcumin. This article explains the latest and detailed study of curcumin and its conjugates, its phytochemistry and biological perspectives and also proved curcumin as an efficient drug candidate for the treatment of numerous diseases. Recent advancements and futuristic viewpoints are also deliberated, which shall help researchers and foster commercial translations of improved nanosized curcumin combination for the treatment of various diseases.

Pharmacophore development, drug-likeness analysis, molecular docking, and molecular dynamics simulations for identification of new CK2 inhibitors

Abstract: Protein kinase 2 (CK2), an essential serine/threonine casein kinase, is considered an interesting target for cancer treatments. Different molecular modeling approaches such as pharmacophore modeling, molecular docking, and molecular dynamics simulations have been used to develop new CK2 inhibitors. This study presents a pharmacophore model that was generated by combining and merging the structure-based and ligand-based pharmacophore features and validated using receiver operating characteristic (ROC). Based on validation results revealing good predictive ability, this pharmacophore model was used as a three-dimensional query in a virtual screening simulation. Several compounds with different chemical scaffolds were retrieved as hits, which were further analyzed and refined using several molecular property filters. The obtained compounds were then filtered and compared to the crystallographic ligand on the basis of their predicted docking energies, binding mode, and interactions with CK2 active site residues. This step resulted in a compound with a high pharmacophore fit value and better docking energy. Molecular dynamics simulation indicated stable binding of the predicted compound to CK2 protein, characterized by root mean square deviation (RMSD) and root mean square fluctuation (RMSF) and hydrogen bond. Graphical abstract.

Synthesis of 2-substituted benzimidazole, coumarin, benzo[b][1,4]oxazin and dihydropyrimidinone derivatives using core-shell structured Fe3O4@SiO2-ZnCl2 nanoparticles as an effective catalyst

Abstract: In this paper, a magnetic nanocatalyst of Fe3O4@SiO2-ZnCl2 has been used which enhances the synthesis of benzimidazoles, coumarins, benzoxazines and dihydropyrimidinones To begin with, 2-substituted benzimidazoles have been synthesized in proper to high yields from 1,2-phenylenediamine with extensive diversity of aromatic aldehydes in the presence of magnetic nanocatalyst Then, this magnetic nanocatalyst has been used for the synthesis of coumarin derivatives via Pechmann condensation reaction of phenols with ethyl acetoacetate in good yield under solvent-free conditions Next, the synthesis of benzo[b][1,4]oxazines has been accomplished efficiently by the multi-component condensation of 2-aminophenol, aromatic aldehyde and isocyanide using magnetic nanocatalyst Lastly, dihydropyrimidinones were synthesized by a one-pot three-component cyclocondensation using β-keto ester, substituted aromatic aldehyde and urea The benefits of this method are facile, easy work-up, catalyst reusability and leading to good yields Theoretical assessments allow us to corroborate the reactions mechanism