The study aimed to synthesize and evaluate the potential anti-inflammatory analgesic activities of rationally designed hybrid molecules imidazolone indole nuclei linked through a methylene bridge. Indolyl-imidazolone hybrids were synthesized in three simple steps starting from 2-phenyl-1 H -indole ( 1 ). In first step, compound was converted -indole-3-carbaldehyde 2 ) using standard conditions ...

Purpose: To evaluate the amino acid, antioxidant and ionic profiles of Carpolobia lutea leaf (Polygalaceae) extract (CLL). Methods: The powdered leaf was macerated and subjected to gradient solvent extraction with nhexane, chloroform, ethyl acetate and ethanol for 72 h to obtain their respective fractions. Amino acid analysis was by cation-exchange chromatography using automated amino acid anal...

The utilization of a photo-induced synthon generated from N-phenyl glycine by an organic dye and visible light irradiation is disclosed. The intermediate could be coupled with either a radical or a nucleophile in a simple operation to afford several natural product-like compounds.

Very few methods for the determination of glycine have been published. Fischer’s method (1) suffers from the usual inadequacies of isolation methods : requiring a large amount of protein, being extremely long and tedious, and yielding only minimal values. Other isolation methods which have been proposed present equally great difficulties. Zimmerman (2) has described a color t.est whereby a viol...

Hepatocytes isolated from sheep were incubated in the presence of reduced phenolics and glycine to determine the effects of these compounds on hepatic propionate metabolism in vitro. 3-Phenyl-propionic (PPA) or t-cinnamic (CA) acids, but not benzoic (BA) or 3-(4-hydroxyphenyl)propionic (4OHPPA) acids, decreased conversion of propionate to glucose at .05 mM in the absence of supplemental glycine...

Several studies have shown that glycine transporter 1 (GlyT1) inhibitors have anxiolytic actions. There are two types of glycine receptor: the strychnine-sensitive glycine receptor (GlyA) and the strychnine-insensitive glycine receptor (GlyB); however, which receptor is the main contributor to the anxiolytic actions of GlyT1 inhibitors is yet to be determined. Here, we clarified which glycine r...

In this research, an efficient synthesis toward 2-(2-((4-Methoxybenzoyl)imino)-4-(4-methoxyphenyl)thiazol-3(2H)-yl)-2-phenylacetic acid via a three-component tandem reaction using aroylisothiocyanate, phenyl glycine, and 4-methoxyphenacyl bromide in an ionic liquid (IL) has been described. 1-Methyl-3-pentylimidazolium bromide (IL) has been employed as a recyclable green solvent. The work-up pro...

The standard glycine site antagonist of the N-methyl-D-aspartate (NMDA) receptor, 3-phenyl-4-hydroxyquinolin-2(1H)-one (21), was used as a template for bioisostere benzene/thiophene exchange. Phenylacetylation of aminothiophene carboxylic acid methyl esters and subsequent cyclization delivered the three possible thienopyridinone isomers. 4-Hydroxy-5-phenylthieno[2,3-b]pyridin-6(7H)-one (3a), wi...

A comparative Hansch type QSAR study was conducted using multiple regression analysis on various sets of quinoxalines, quinoxalin-4-ones, quinazoline-2-carboxylates, 4-hydroxyquinolin-2(1H)-ones, 2-carboxytetrahydroquinolines, phenyl-hydroxy-quinolones, nitroquinolones and 4-substituted-3-phenylquinolin-2(1H)-ones as selective glycine/NMDA site antagonists. Ten statistically validated equations...