Fluorination is a useful tool in medicinal chemistry. It is also increasingly applied in the field of peptide and protein engineering to address its unique challenges. The development of synthetic approaches toward fluorinated analogs of aminobutyric acid, valine, leucine, and isoleucine, descri...

Publisher SummaryThis chapter describes the parallel inhibitions by 4-pentenoic acid of fatty acid oxidation and the two thiolases present in rat heart mitochondria. Experiments with purified 3-ketoacyl-CoA thiolase demonstrate that this enzyme is most rapidly inactivated by 3-keto-4-pentenoyl-C...

The main objective of this work was to evaluate a comprehensive two-dimensional gas chromatographic (GCxGC) coupled to quadrupole mass spectrometry (qMS) method in the field of biomarker candidates’ discovery. To this purpose we developed a GCxGC-qMS method suitable for the separation of organi...

The detailed synthesis of (bis)aminoacyl-pdCpAs and the corresponding singly and tandemly activated tRNAs is reported. The synthetic pathway leading to these compounds has been validated for simple amino acid residues as well as for amino acids bearing more complex side chains. Protection/deprot...

Microorganisms are believed to be a promising feedstock for the production of many by-products (lactic acid, single cell proteins, bioethanol, polyunsaturated fatty acids) that can resolve the putative problems and cover a wide range of industrial applications. Among these components, polyhydrox...

Since its extensive development in the early 1980s, SFE has attracted considerable attention as a sample-preparation procedure. However, other different sample preparation procedures, including precipitation, liquid- and/or solid-phase extraction in biological fluids, also remain in use. In this...

The objective of the study was to evaluate the in vitro activity of orbifloxacin against Staphylococcus intermedius strains isolated in France from canine skin and ear infections. The minimum inhibitory concentrations (MICs) of orbifloxacin against 240 field S. intermedius isolates (69 skin and ...

The single-dose disposition kinetics of orbifloxacin were determined in clinically normal lactating goats (n = 6) after intravenous, subcutaneous, and intramuscular administration of 2.5 mg of orbifloxacin/kg of body weight. Orbifloxacin concentrations were determined by HPLC with fluorescence d...

IntroductionSingle-dose pharmacokinetics of orbifloxacin (2.5 mg/kg body weight) were determined in clinically normal female Patanwadi sheep (n = 6) following intravenous and intramuscular administration.

1-(2-Furylmethyl)-2,2,5,5-tetramethyl-1-aza-2,5-disilacyclopentane 3a was reacted sequentially with t-butyllithium, an aldehyde and hydrochloric acid to produce the corresponding 6-substituted 3-pyridinol.

Prion diseases are fatal neurodegenerative disorders of the central nervous system characterized by the accumulation of a protease resistant form (PrPSc) of the cellular prion protein (PrPC) in the brain. Two types of cellular prion (PrPC) compounds have been identified that appear to affect pri...

Penile erection induced by α-melanocyte-stimulating hormone and melanocortin receptors (MC-R) in areas of the spinal cord and periphery has not been demonstrated. To elucidate sites of the proerectile action of melanocortin peptides, in awake male rats we administered the MC-R agonist Ac-Nle-c[...

The melanocortin-4 receptor (MC4R) acts as a member of G-protein coupled receptors and participate in food intake and energy expenditure. Melanocortin 2 receptor accessory protein 2 (MRAP2) plays a critical role in regulating MC4R signaling in mammals and zebrafish. However, evidence on their in...

A benign, simple, and efficient synthesis of 4-alkyl-5-methyl-1H-pyrazol-3-ols has been described in refluxing water through the four-component reaction of β-ketoesters, hydrazine hydrate, different aldehydes, and acetophenone derivatives in the presence of nano Al2O3@Cg, as a novel nanocatalys...

This chapter discusses pyrolysis of a variety of compounds containing carboxyl groups. This include monocarboxylic acids such as formic, acetic, homologs and substituted acetic acids, acids with α,β-unsaturation and β,γ-unsaturation, and several aromatic monocarboxylic acids. The discussion ...

The kinetics of Ca2+ release induced by the second messenger D-myoinositol 1,4,5 trisphosphate (IP3), by the hydrolysis-resistant analogue D-myoinositol 1,4,5 trisphosphorothioate (IPS3), and by micromolar Ca2+ were resolved on a millisecond time scale in the junctional sarcoplasmic reticulum (S...

The effectiveness of the nonmetabolizable second messenger analogue DL-myo-inositol 1,4,5-trisphosphorothioate (IPS3) described by Cooke, A. M., R. Gigg, and B. V. L. Potter, (1987b. Jour. Chem. Soc. Chem. Commun. 1525–1526.) was examined in triads purified from rabbit skeletal muscle. A Ca2+ e...

The equilibrium and kinetic binding characteristics of D-inositol 1,4,5-trisphosphate (Ins(1.4.5)P3) have been studied in membrane preparations of rat cerebellum and bovine adrenal cortex. Saturation analysis of isotopic dilution binding data demonstrated apparent KD values for Ins(1,4,5)P3 bind...

In single mouse pancreatic acinar cells the effects of intracellular infusion of inositol 1,4,5-trisphosphate (InsP3) or the non-metabolizable InsP3 analogue inositol 1,4,5-triphosphorothioate (InsPS3) have been investigated using a wide range of concentrations. Different types of cytosolic Ca2+...

H-Phosphinic acid and its esters can be considered as derivatives of hypophosphorous acid and its esters in which one of the P–H bonds is replaced by PC bond. Methods for preparation of H-phosphinic acid, its esters and α-amino H-phosphinic acid, and characteristic reactions of P–H group of t...