The 1,3-dipolar cycloaddition reactions of various N-tethered alkenyl aldehydes with some cyclic and acyclic amino acids have been studied. Some key sulfonamides having strategically positioned aldehyde and olefinic tether have been synthesized and effectively subjected to intramolecular azometh...

The inhibitory actions of phenylbutazone, oxyphenbutazone and γ-hydroxyphenylbutazone on the growth of human bone marrow granulocyte/monocyte colonies in vitro have been compared. Oxyphenbutazone is more toxic than phenylbutazone in this system, γ-hydroxyphenylbutazone is inhibitory over a wid...

The permeation rate of phenylbutazone through membranes of polydimethylsiloxane and everted rat intestine was measured over a range of pH values. The classical pH-partition hypothesis was not obeyed. Permeability coefficients were calculated using a modification of Higuchi's general equatio...

The objective was to compare the gastrointestinal and general toxicity of suxibuzone (SBZ) to that of phenylbutazone (PBZ) when administered orally in horses. Fifteen healthy horses were allocated to three treatment groups. One group received a high dose of PBZ for two weeks; the second group wa...

This work describes a simple screening protocol for quantification of carbasalate calcium derived metabolites, acetylsalicylic acid (ASA) and salicylic acid (SA), in animal and aquatic food matrices using liquid chromatography-tandem mass spectrometry (LC-MS/MS). The analytes were extracted from...

Interference or “masking” in thin layer chromatography occurs when the presence of one drug on a thin layer plate physically obscures or interferes with the detection of another drug. We investigated the ability of phenylbutazone and oxyphenbutazone to mask or interfere with the detection of a...

1.1. The interference of propylene glycol with anti-inflammatory effects of phenylbutazone was investigated.2.2. Inhibitory effect of phenylbutazone on both carrageenin-induced edema and the cotton pellet granuloma was increased when propylene glycol was used as solvent.3.3. Propylene glycol giv...

Phenylbutazone (PhB) is a powerful anti-inflammatory drug that is very sparsely soluble in water (solubility ≌ 1 × 10−3M). This drug is capable of altering the phase transition temperature of phospholipid bilayers consisting of pure dimyristoyl- or dipamitoyl phosphatidylcholine without changi...

Phenylbutazone (PhB) is a powerful anti-inflammatory drug that is very sparingly soluble in water (solubility ⋍ 1 × 10−3M). This drug is capable of altering the phase transition temperature of phospholipid bilayers consisting of pure dimyristoyl- or dipalmitoylphosphatidylcholine without changi...

The effect of feeding Sporobolus and Rhodes hay on phenylbutazone (4 g) relative absorption was examined in six camels using a two-period, two-sequence, two-treatment crossover design. Serum concentration of the drug was measured by high performance liquid chromatography. The measured values (me...

Two methods for the synthesis of 4-acetylamino benzoic acids substituted at the 3-position with imidazoles are described. Many of the compounds are inhibitors of influenza virus sialidases with levels of activity similar to the recently described 4-acetylamino-3-guanidino-benzoic acid (BANA 113).

The rhodium-catalyzed asymmetric hydrogenation of β-acetylamino acrylonitriles was investigated by using monophosphine and bisphosphine ligands. It was found that an Rh-QuinoxP∗ complex exhibited high enantioselectivities for β-aryl substituted β-acetylamino acrylonitriles and the Rh-JosiPhos...

A series of novel 4-phenoxyquinoline derivatives containing 3-oxo-3,4-dihydroquinoxaline moiety were synthesized and evaluated for their c-Met kinase inhibitory activity and antiproliferative activity against five cancer cell lines (HT-29, H460, A549, MKN-45 and U87MG) in vitro. Most of the comp...

A series of 6,7-disubstituted-4-(2-fluorophenoxy)quinoline derivatives possessing 1,2,3-triazole-4-carboxamide moiety were designed, synthesized and evaluated for their in vitro biological activities against c-Met kinase and five typical cancer cell lines (A549, H460, HT-29, MKN-45 and U87MG). M...

A series of 4-(2-fluorophenoxy)quinoline derivatives containing an imidazolone moiety were designed, synthesized and evaluated for their in vitro biological activities against c-Met kinase and four cancer cell lines (A549, H460, HT-29 and MKN-45). Most compounds showed moderate to excellent acti...

A series of novel 4-(2-fluorophenoxy)quinoline derivatives containing 4-oxo-1,4-dihydrocinnoline-3-carboxamide moiety were designed, synthesized and evaluated for their in vitro biological activities against c-Met kinase and six typical cancer cell lines (A549, H460, HT-29, MKN-45, U87MG and SMM...

Six series of novel 4-(2-fluorophenoxy)-3,3′-bipyridine derivatives conjugated with aza-aryl formamide/amine scaffords were designed and synthesized through a structure-based molecular hybridization approach. The target compounds were evaluated for c-Met kinase inhibitory activities and cytotox...

A series of 6,7-disubstituted-4-(2-fluorophenoxy)quinoline derivatives possessing 1,2,3-triazole-4-carboxamide moiety were designed, synthesized and evaluated for their in vitro cytotoxic activities against four typical cancer cell lines (A549, H460, HT-29, and MKN-45). Most compounds showed mod...

Two novel series of 6,7-disubstituted-4-(2-fluorophenoxy)quinoline derivatives bearing 1H-imidazole-4-carboxamido or (E)-3-hydrosulfonylacrylamido motifs (16–31 and 32–42) were designed, synthesized and evaluated for their in vitro cytotoxic activity. Most of the compounds exhibited moderate t...

Four 3-(methylsulfanyl)propionate esters, ethyl 3-(methylsulfanyl)prop-2-enoate, two 2-(methylsulfanyl)acetate esters and their possible precursors 2-(methylsulfanyl)ethanol, 3-(methylsulfanyl)propanol and 3-(methylsulfanyl)propanal were quantified from the headspace of Actinidia chinensis ‘Hor...