Microwave-assisted organic reactions have been applied as an effective technique in organic synthesis. Microwave irradiation often leads to shorter reaction times, increased yields, easier workup, matches with green chemistry protocols, and can enhance the region and stereo selectivity of reactions. In fact, the high usefulness of microwave-assisted synthesis encouraged us to increase the efficiency of several organic transformations and synthesis. High-speed microwave-assisted chemistry has attracted a considerable amount of attention in recent years and has been applied successfully in various fields of synthetic organic chemistry, proteins, peptides, drug discovery, and green chemistry. The various roles of microwaveassisted organic chemistry in green and sustainable chemistry are discussed, beginning with the strategies, technologies, and methods that were employed routinely at the time of the first reports of microwave applications. Microwave processing has several advantages over conventional sintering/heating, such as the reduction in cycle time, energy efficiency, eco-friendliness, and providing finer microstructures, leading to improved mechanical properties. Herein, we also describe the evolution of the microwave and some early applications of microwave assistance in the biomolecular sciences and treatment of solid malignant tumors.
Synthesis and biological activity of some new 1-benzyl and 1-benzoyl-3-heterocyclic indole derivativesStarting from 1-benzyl- (2a) and 1-benzoyl-3-bromoacetyl indoles (2b) new heterocyclic, 2-thioxoimidazolidine (4a, b), imidazolidine-2,4-dione (5a, b), pyrano(2,3-d)imida-zole (8a, band9a, b), 2-substituted quinoxaline (11a, b-17a, b) and triazolo(4,3-a)quinoxaline derivatives (18a, band19a, b) were synthesized and evaluated for their antimicrobial and anticancer activities. Antimicrobial activity screening performed with concentrations of 0.88, 0.44 and 0.22 μg mm-2showed that 3-(1-substituted indol-3-yl)quinoxalin-2(1H)ones (11a, b) and 2-(4-methyl piperazin-1-yl)-3-(1-substituted indol-3-yl) quinoxalines (15a, b) were the most active of all the tested compounds towardsP. aeruginosa, B. cereusandS. aureuscompared to the reference drugs cefotaxime and piperacillin, while 2-chloro-3-(1-substituted indol-3-yl)quinoxalines (12a, b) were the most active against C.albicanscompared to the reference drug nystatin. On the other hand, 2-chloro-3-(1-benzyl indol-3-yl) quinoxaline12adisplay potent efficacy against ovarian cancer xenografts in nude mice with tumor growth suppression of 100.0 ± 0.3 %.
In recent years, molecular modeling has become an important technique for drug discovery and pharmaceutical science. The objective of this study is to determine the molecular modeling of the antibacterial, anti-inflammatory and anti-nociceptive activities of a new series of pyrazoles, oxadiazoles and sugar hydrazines of 5-nitroindolin-2-one derivatives. The molecular modeling protocol was applied using the MOE (Molecular Operating Environment) software. Synthetic compounds 1, 3, 8, 9, 10 and 12 were the most active compounds, as antibacterial, antiinflammatory and anti-nociceptive activities were studied for the binding affinity of the cyclooxygenase1 (COX1), The glucocorticoid receptor (GR), the cytochrome P450 receptor of 14alfa-sterol demethylases (CYP51) and the dihydroprotease synthase receptor. Molecular modeling studies revealed that the [(methylbenzyl)-5-nitro-2-oxoindolin-3-ylideneamino-benzohydrazide derivative (3) gave a score of (-15.8587 kcal/mol), while 1,3,4-oxadiazol-2-yl) phenylimino)-1-(methylbenzyl)-5-nitroindolin-2-one derivative (9) gave a higher score (-16.8038 kcal/mol) than flucanazole Co-crystallized gave a score of (-10.2837 kcal/mol). However, the compound (12), D-Arabinose-(methylbenzyl)-5-nitro-2-oxoindolin-(3-ylideneamino) hydrazone derivative gave a score of (-24.6577 kcal/mol) greater than the co-crystallized ligand which gave a score of (-16.6717 kcal/mol).
In drug discovery and development, the quantification of drugs in biological samples is an important task for the determination of the physiological performance of the investigated drugs. After sampling, the next step in the analytical process is sample preparation. Because of the low concentration levels of drug in plasma and the variety of the metabolites, the selected extraction technique should be virtually exhaustive. Recent developments of sample handling techniques are directed, from one side, toward automatization and online coupling of sample preparation units. The primary objective of this review is to present the recent developments in microextraction sample preparation methods for analysis of drugs in biological fluids. Microextraction techniques allow for less consumption of solvent, reagents, and packing materials, and small sample volumes can be used. In this review the use of solid phase microextraction (SPME), microextraction in packed sorbent (MEPS), and stir-bar sorbtive extraction (SBSE) in drug analysis will be discussed. In addition, the use of new sorbents such as monoliths and molecularly imprinted polymers will be presented.
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