Combinatorial Chemistry & High Throughput Screening - Volume 20, Issue 9, 2017

Aim and Objective: 4-Hydroxyphenylpyruvate dioxygenase (HPPD), converting phydroxyphenylpyruvate (HPPA) to homogentisate (HGA), is an important target for treating type I tyrosinemia and synthesizing novel herbicides due to its significant role in tyrosine catabolism. Hence, it is imperative to design novel HPPD inhibitors that can block HPPA–HGA conversion, which leads to the deficiency in isoprenoid redox cofact Read More

Background: Anthocephalus cadamba is used in traditional and folklore medicinal system. Objectives: In order to validate its traditional medicinal claim, the present study was designed to assess antioxidant, antigenotoxic and cytotoxic activity of fractions from Anthocephalus cadamba bark and to identify their active phytoconstituents. Methods: The four fractions viz. hexane (HACB), chloroform (CACB), ethylacetate (EACB) a Read More

Aims and Objectives: The importance of acridine core structure and other heterocycles containing its framework is well known, as they are found in numerous compounds with a variety of biological effects. Pyridine is also an important solvent and heterocyclic nucleus for the design and synthesis of novel molecules with biological properties. It occurs in several natural compounds which are used as a precursor in agrochemicals an Read More

Objective: Functionalized benzenes are prepared from the reaction of sulfonoketenimides that is produced from the Copper catalyzed reaction of terminal alkynes and sulfonyl azides with zwitterionic intermediate that is generated from the reaction of dialkyl acetylenedicarboxylates, alkyl bromides and triphenylphosphine in the presence of ZnO-nanoparticles in good yields. Material and Methods: All chemicals employed in Read More

Objective: Palladium nanoparticles (Pd NPs) supported on the TiO2 NPs were prepared using Euphorbia thymifolia L. leaf extract. The Pd/TiO2 NPs were characterized by FESEM, EDS, TEM and XRD analysis and were used as nanocatalysts for the reduction of a variety of organic dyes. To the best of the author’s knowledge, this study explains the first report to the synthesis of Pd/TiO2 NPs using Euphorbia thymifolia L. leaf extr Read More

Aim and Objective: Mitragynine, a major active alkaloid of Mitragyna speciosa, acts as an agonist on μ-opioid receptors, producing effects similar to morphine and other opioids. It has been traditionally utilized to alleviate opiate withdrawal symptoms. Besides consideration about potency and selectivity, a good drug must possess a suitable pharmacokinetic profile, with suitable absorption, distribution, metabolism, excretion an Read More

Objective: Herein we demonstrate the successful development of a new RORγt-enhanced IL-17F promoter-luciferase reporter assay and its use in a parallel high throughput screening approach, alongside a RORγt TR-FRET assay, to rapidly identify new small molecule RORγt/IL-17 inhibitors and evaluate their mode of action. Material & Methods: We sought to identify cell-permeable small-molecule inhibitors of RORγt for rapid pro Read More

Background: One key step in the development of inhibitors for an enzyme is the application of computational methodologies to predict protein-ligand interactions. The abundance of structural and ligand-binding information for HIV-1 protease opens up the possibility to apply computational methods to develop scoring functions targeted to this enzyme. Objective: Our goal here is to develop an integrated molecular docking a Read More