Two highly potent and selective cystic fibrosis (CF) transmembrane regulator (CFTR) inhibitors have been identified by high-throughput screening: the thiazolidinone CFTR(inh)-172 [3-[(3-trifluoromethyl)phenyl]-5-[(4-carboxyphenyl)methylene]- 2-thioxo-4-thiazolidinone] and the glycine hydrazide GlyH-101 [N-(2-naphthalenyl)-((3,5-dibromo-2,4-dihydroxyphenyl)methylene)glycine hydrazide]. Inhibitio...

Reaction of sodium salt of allyl alcohol with 2-chloro-5-phenyl- l,3,4-thiadiazole gave 2-allyloxy-5-phenyl-1,3,4-thiadiazole 2. Compounds 4a and 4b could be obtained through the reaction of nitrone 3 with 2. Reaction of compound 2 with nitrone 5 afforded the final compound 6. Antifungal activity of all compounds was less than ketoconazole

Free glycine is known to have vital functions in the mammalian brain, where it serves mainly as both neurotransmitter and neuromodulator. Despite its importance, little is known about the metabolic pathways of glycine synthesis and degradation in the central nervous system. In this study, the pathway of glycine metabolism in astroglia-rich primary cultures from rat brain was examined. The cells...

1. Total RNA isolated from embryonic chick paravertebral sympathetic ganglia was used in a reverse transcription-polymerase chain reaction (RT-PCR) assay with a pair of degenerate oligonucleotide primers deduced from conserved regions of mammalian glycine receptor alpha-subunits. Three classes of cDNA were identified which encode portions of the chicken homologues of the mammalian glycine recep...

Seven lines of haploid Nicotiana tabacum tissue culture selected for resistance to normally toxic levels of the glycine analog glycine hydroxamate, a competitive inhibitor of the glycine decarboxylase reaction, were investigated. The presence of glycine hydroxamate greatly increased the intracellular concentration of both glycine and alanine in wild type and resistant cell lines, suggesting tha...

In many bacterial species, the glycine riboswitch is composed of two homologous ligand-binding domains (aptamers) that each bind glycine and act together to regulate the expression of glycine metabolic and transport genes. While the structure and molecular dynamics of the tandem glycine riboswitch have been the subject of numerous in vitro studies, the in vivo behavior of the riboswitch remains...

Accumulation of (14)C-labeled glycine and microelectrode techniques were employed to study glycine transport and the effect of glycine on the membrane potential (Deltapsi) in Lemna gibba G1. Evidence is presented that two processes, a passive uptake by diffusion and a carrier-mediated uptake, are involved in glycine transport into Lemna cells. At the onset of active glycine uptake the component...

The formation constants of the species formed in the systems fr + glycine + dioxovanadium(V) + and H+ + glycine have been determined in aqueous solutions of methanol at 25 °C and constant ionicstrength, using spectrophotometric and potentiometric techniques. It was shown thatdioxovanadium(V) forms two mononuclear 1 : land 1:2 complexes with glycine. The formationconstants in various media were ...