(Z)-3-XCH2-4-(C6H5)-3-buten-2-one enones (X = SCN, N3, SO2Me, OC6H5) were synthesized and submitted to biotransformations using whole Saccharomyces cerevisiae cells. The enone (X = SCN) produced (R)-4-(phenyl)-3-methylbutan-2-one (R)-6 with 93% ee and enones (X = N3, SO2Me, OC6H5) yielded a mixt...

(1-Diphenylphosphino)cyclopropanecarbonitrile 1 was synthesised by the reduction of a phosphine oxide; the interaction of 1 with (PhCN)2PdCl2 leads to 1:1 or 1:2 complexes depending on the ratio between the reactants.

A large number of carboximides have been synthesized, tested and, in some cases, marketed as agricultural fungicidal agents. One carboximide fungicide N-(3,5-dichlorophenyl)succimide (NDPS) proved to be both highly efficacious as a fungicide and a nephrotoxin. The purpose of this study was to co...

Although the addition of chloride groups to the phenyl ring of N-phenylsuccinimide (NPS) is known to enhance the nephrotoxic potential of NPS, the mechanism of this enhancement is unknown. One chlorinated NPS derivative, N-(3,5-dichlorophenyl)succinimide (NDPS), is a potent nephrotoxicant which ...

N-(3,5-Dichlorophenyl)succinimide (NDPS) is an agricultural fungicide which induces acute tubular necrosis as its primary toxicity. Two NDPS metabolites, N-(3,5-dichlorophenyl)-2-hydroxysuccinimide (NDHS) and N-(3,5-dichlorophenyl)-2-hydroxysuccinamic acid (NDHSA) previously have been shown to b...

The successful clinical management of lung cancer is limited by frequent loss-of-function mutations in p53 which cooperates with chronic oxidant-stress induced adaptations in mercapturic acid pathway (MAP) which in turn regulates critical intracellular signaling cascades that determine therapeut...

The agricultural fungicide N-(3,5-dichlorophenyl)succinimide (NDPS) induces nephrotoxicity characterized as polyuric renal failure and mediated via metabolites arising from oxidation of the succinimide ring. Recent findings have suggested that the stereochemical nature of NDPS metabolites may be...

The agricultural fungicide N-(3,5-dichlorophenyl)succinimide (NDPS) produces kidney damage in rats. Although many NDPS analogues have been screened as possible nephrotoxicants, the one-carbon homologue, N-(3,5-dichlorophenyl)glutarimide (NDPG), has not been evaluated. This study examined the nep...

Cytochrome P450 (CYP)-mediated metabolism in the thiazolidinedione (TZD) ring may contribute to the hepatotoxicity of the insulin-sensitizing agents such as troglitazone. We were interested in determining if biotransformation could also be a factor in the liver damage associated with another TZD...

Nephrotoxicity of the agricultural fungicide N-(3,5-dichlorophenyl)succinimide (NDPS) in rats is believed to involve metabolism on the succinimide ring. To further investigate this hypothesis, we synthesized and tested the following NDPS analogues, which contain other cyclic imide rings and may ...

The agricultural fungicide N-(3,5-dichlorophenyl)succinimide (NDPS) can induce marked nephrotoxicity in rats following a single intraperitoneal (ip) administration of 0.4 mmol/kg or greater. Although NDPS induces direct renal proximal tubular toxicity, a role for renal vascular effects may also ...

The thiazolidinedione (TZD) ring is a constituent of the glitazones that are used to treat type II diabetes. Liver injury has been reported following chronic glitazone use; however, they do not produce hepatic damage in common laboratory animal species. In contrast, 3-(3,5-dichlorophenyl)-2,4-th...

Synthesis of 7-(4-bromobutoxy)-5-hydroxy-2-phenyl-4H-chromen-4-one intermediate treating chrysin with 1,4-dibromobutane facilitated combination of chrysin with a wide range of piperazine moieties which were equipped via reacting the corresponding amines with bis(2-chloroethyl)amine hydrochloride...

An intravenous injection of the contrast medium Meglumine Ioglycamide (Biligram) led to a fatal incident in a patient (E.O.) suffering from Macroglobulinemia Waldenström. Subsequently the interaction of IgME.O. with mono- and divalent drugs bearing the antigenic determinant 3-amino-2,4,6-triiodo...

From the previous paper we have evidence for an antigen-antibody-like reaction being the basic mechanism in the binding of the divalent contrast media Ioglycamide and Iodipamide to the monoclonal paraprotein IgME.O.. The influence of length and chemical structure of the linking chains of various...

The synthesis and biological evaluation of a series of novel 3-phenylpiperidine-4-carboxamide derivatives are described. These compounds are generated by hybridization of the substructures from two types of tachykinin NK1 receptor antagonists. Compound 42 showed high metabolic stability and exce...

A novel series of 2-(phenoxyaryl)-3-urea derivatives were designed, synthesized, and biologically evaluated for their anti-thrombotic activity. Most of compounds exhibited good inhibition against P2Y1 receptor. Among them, three compounds 11, 12, and 13 demonstrated good P2Y1 receptor antagonist...

Further exploration around the recently disclosed potent triple re-uptake inhibitor 6-(3,4-dichlorophenyl)-1-[(methyloxy)methyl]-3-azabicyclo[4.1.0]heptane led to the identification of a new series of potent triple re-uptake inhibitors endowed with good developability characteristics. The insert...

Three new compounds, N-(3,4-dichlorophenyl)-N′-(2-methylbenzoyl)thiourea (2a), N-(3,4-dichlorophenyl)-N′-(3-methylbenzoyl)thiourea (2b) and N-(3,4-dichlorophenyl)-N′-(4-methylbenzoyl)thiourea (2c) are isomers which have been successfully synthesised and characterised by typical spectroscopic ...

The mode of action of the antiviral drug 5-(3,4-dichlorophenyl) methylhydantoin (hydantoin) was studied in a cell-free system allowing de novo synthesis of poliovirus. This cell-free system, which is programmed with viral RNA, is suitable for the study of the late stages of poliovirus replicatio...