In this investigation, a series of 1-phenyl-3-(5-(pyrimidin-4-ylthio)-1,3,4- thiadiazol-2-yl)urea receptor tyrosine kinase inhibitors were synthesized by a simple and efficient structure-based design. Structure-activity relationship (SAR) analysis of these compounds based on cellular assays led ...

The corrosion inhibition properties of novel cationic surfactant on carbon steel in 7 M H3PO4 solution have been determined by weight loss, Tafel polarization and electrochemical impedance spectroscopy (EIS) methods. The results revealed that the synthesized cationic surfactant is a good corrosi...

Although there is a variety of biological activity reports regarding compounds derived from thiazolidin-4-ones, no data related to ovicidal activity against trematodes, particularly Fasciola hepatica are available. Since there are reports about anthelmintic resistance in F. hepatica, new drugs a...

A variety of chroman-4-one and indanone derivatives were conveniently synthesized from readily available cyclopropanols and alkenyl aldehydes via a silver catalyzed radical ring-opening/coupling/cyclization cascade. The reaction proceeded under mild and neutral conditions with broad substrate sc...

Seven 3,5-dihydroxy-7,8-dimethoxyflavones were synthesized from the corresponding 3,5,7,8-tetramethoxyflavones using selective demethylation and protection of 3- or 5- methoxy group, and their properties were clarified by the UV and 1H NMR spectral data. The structures of the four natural flavon...

Treatment of 1,6:2,5-dianhydro-3,4-di-O-methanesulfonyl-1-thio-d-glucitol in methanol with sodium hydroxide afforded 1,6:2,5:3,4-trianhydro-1-thio-allitol, 1,4:2,5-dianhydro-6-methoxy-1-thio-d-galactitol, 1,6:2,5-dianhydro-4-O-methyl-1-thio-d-glucitol, 1,6:2,5-dianhydro-3-O-methanesulfonyl-1-thi...

Photocatalytic degradation of paraoxon-ethyl (o,o-diethyl o-(4-nitrophenyl) phosphate), a well known surrogate of chemical warfare agents, in aqueous solution was studied by using titania nanoparticulate film. Reaction followed pseudo first order behaviour. Photolytic degradation reaction of par...

Over the last 30 years, (±)-1-(9-fluorenyl)ethyl chloroformate ((±)-FLEC) was used as a chiral derivatizing agent in various analytical applications involving a wide range of endogenous, pharmaceutical and environmentally relevant molecules.This comprehensive review aims to present all the sig...

Glycosylation (catalyzed by mercuric cyanide) of p-nitrophenyl 2,4,6-tri-O-acetyl-β-d-galactopyranoside (2) with 2,3,4,6-tetra-O-acetyl-α-d-galactopyranosyl bromide in acetonitrile afforded the α-(1→3)- and β-(1→3)-linked disaccharide heptaacetates (4 and 6, respectively) in almost equal p...

Thioglycosides have proved to be useful, enzymatically stable analogs of glycosides for structural and mechanistic studies and their synthesis is considerably simplified through the use of thioglycoligases. As part of an investigation into the use of thioglycosides as potential pharmacological c...

A series of [2-imidazol-1-yl-2-(6-alkoxy-naphthalen-2-yl)-1-methyl-ethyl]-dimethyl-amines were designed and synthesized as CYP26 inhibitors, serving as retinoic acid metabolic blocking agents (RAMBA’s).

C-terminal fragment of bovine κ-casein contains glycosidic residues. There are several glycoforms of κ-casein containing different kinds and numbers of glycosidic residues. Such heterogeneity affects properties of this protein and its fragments.The C-terminal fragment of cow's κ-casein (...

Publisher SummaryThis chapter describes the evaluation of sometribove in toxicology and clinical trials in Europe and the United States. Somatotropin purified from bovine pituitary glands consistently increases milk yields when administered to lactating dairy cows. High doses of sometribove were...

During summer, 34 cows received daily injections of placebo or 25 mg of bST and were placed in a thermoregulated or a heat stress environment. Heat stress increased rectal temperatures, respiration rates, and plasma cortisol concentrations and decreased milk yield. Four of 9 bST-treated cows and...

Three distinct antigenic regions of bovine somatotropin (bST) were identified on the basis of the ability of a set of monoclonal antibodies to bind to proteolytic fragments and deletion variants of recombinant bST (rbST) in Western blot analyses. One of the regions is further subdivided into two...

In Experiment 1, an SC injection of 14 μg CRH greatly suppressed the vocalizing of isolated guinea pig pups 1 h later and produced highly elevated plasma cortisol levels. In Experiment 2, SC injection of 18 international units of ACTH produced similar cortisol elevations, but had a negligible e...

1.1. In adipose slices of the guinea pig (Cavia porcellus), adrenocorticotrophic hormone (ACTH) produced a significantly higher lipolytic response (increased Vmax and decreased Km) as compared to norepinephrine (NE), thus indicating a marked difference with human adipose tissue.2.2. Exercise-tra...

The guinea-pig has high levels of circulating cortisol. Though adrenocorticotropin (ACTH) levels are similar to those in other mammals, guinea-pig ACTH has been reported to have a single amino-acid substitution which results in increased bioactivity of the peptide. Pro-opiomelanocortin (POMC) is...

Peripheral treatment with adrenocorticotropin (1–24) (ACTH1–24), at different doses and sequences, consistently antagonized the decrease in body temperature produced by morphine in the freely moving guinea pig, whereas adrenocorticotropin (4–10) (ACTH4–10), which lacks corticotrophic activit...

Guinea-pig ACTH has been found to be distinct from other mammalian ACTHs in having an alanine for proline substitution at position 24 and in having superagonist aldosterone-stimulating activity relative to synthetic ACTH(1–24) in an isolated rat glomerulosa cell bioassay. We have purified ACTH ...