in the present study, aqueous solutions of some copper-complexing ligands were screened for their cytotoxicity using brine shrimp lethality test. among the ligands tested, diacetyl-bis(n4-methylthiosemicarbazones) (atsm) proved to be the most safe and non-toxic compound (2% lethality at 10 ppm), while pyruvaldehyde bis(n4-methyl)thiosemicarbazone (ptsm) was shown to possess low toxicity (7% let...

The fluorous traceless synthesis of substituted indole alkaloids is carried out first by attaching the 3-(perfluorooctyl)propanol with Boc protected L-tryptophan. The reaction of perfluoroalkyl (Rfh)-tagged tryptophan esters with various aldehydes undergoes Pictet-Spengler reaction to give cis and trans stereoisomers of tetrahydro-beta-carbolines. The nucleophilic addition of the piperidine nit...

The relative stability of the different tautomers of hydantoin has been studied through the use of DFT method. The structures and the vibrational frequencies of all stable tautomers and all the transitions states connecting between them have been calculated at the B3LYP/6-311+G(d,p) level of theory in the gas phase and selected solvents using IE-PCM model. Final energies have been obtained in s...

The anticonvulsant diphenylhydantion (DPH) causes embryonic folate antagonism in the animal model of the fetal hydantoin syndrome. Thus, comparisons were made between the metabolic effects of the teratogens DPH and 9-methyl pteroylglutamic acid (9-methyl PGA), a folate antagonist. The DPH inhibited ornithine decarboxylase (ODC), the rate-limiting enzyme in putrescine biosynthesis, and caused re...

Daily administration of sodium biphenyl hydantionate (Dilantin) to rats has been shown to increase markedly the dermal concentration of insoluble collagen and non-collagenous protein (1) as well as to decrease the concentration of both tissue water and fat (2). These effects were produced by ten or more daily doses of 100 mg of drug per kg body weight (3) and were a result of the specific struc...

INTRODUCTION Planorbis planorbis (Ram's Horn Snail) is a species of air-breathing freshwater snail, an aquatic gastropod mollusk in the family Planorbidae. It is one of the most common freshwater snails in Europe, occurs in numerous water body types with a preference for standing water such as ponds, swamps or lakes with slow moving or stagnant waters. As typical freshwater invertebrate it is c...

4-Hydroxyphenylmethylene hydantoin (PMH, 1), isolated from the Red Sea sponge Hemimycale arabica, and delta-tocotrienol (3), isolated from the tocotrienol-rich fraction of palm oil, are important antimetastatic and antiproliferative natural products that proved effective against metastatic prostate and breast cancers, respectively. New fluorescent derivatives of PMH (2) and delta-tocotrienol (4...

Dissolution behaviour of both 5, 5-diphenyl hydantoin sodium commonly known as dilantin sodium (DS) and its corresponding marketed capsule dilantin have been studied in aqueous as well as micellar media. Percentage dissolution of both DS and its marketed capsule are found to be low as expected in aqueous medium due to its very low solubility in water. However, their dissolution tendency is foun...

A quantitative structure property relationship investigation was performed on the lipophilicities of a number of hydantoin derivatives as measured by the RP-HPLC retention times provided by Scholl et al. (Scholl, S.; Koch, A.; Henning, D.; Kempter, G.; Kleinpeter, E. Struct. Chem. 1999, 10, 355-366). The lipophilicities (S) were correlated with the theoretical molecular descriptors of the hydan...