Multidrug resistance has become a factor seriously limiting treatment of various diseases, including bacterial (1ñ3) and fungal (4) infections and cancer (5ñ7). The major mechanism of multidrug resistance (MDR) in cancer is the over-expression of ATP-dependent drug-efflux pumps (drug transporters), which reduces the accumulation of agents. One of the most important mechanisms of MDR in cancer i...

In 1912 Lewis (1) administered hydantoin to rabbits, cats, and dogs and came to the conclusion that the ring was not readily broken in the body. Gaebler and Keltch (2) some years later showed that some hydantoin was excreted as hydantoic acid after injection into dogs. Wada (3) claimed that urea was produced from hydantoin after incubation with milk or certain tissue suspensions. Finally, Kozel...

The gene hyuP from Microbacterium liquefaciens AJ 3912 with an added His6 tag was cloned into the expression plasmid pTTQ18 in an Escherichia coli host strain. The transformed E. coli showed transport of radioisotope-labeled 5-substituted hydantoins with apparent K(m) values in the micromolar range. This activity exhibited a pH optimum of 6.6 and was inhibited by dinitrophenol, indicating the r...

The hydantoin racemase gene of Pseudomonas sp. strain NS671 had been cloned and expressed in Escherichia coli. Hydantoin racemase was purified from the cell extract of the E. coli strain by phenyl-Sepharose, DEAE-Sephacel, and Sephadex G-200 chromatographies. The purified enzyme had an apparent molecular mass of 32 kDa as determined by sodium dodecyl sulfate-polyacrylamide gel electrophoresis. ...

Hydantoin derivatives are commonly used anticonvulsants. In general, they effective for partial-onset seizures and tonic-clonic seizures, but not absence seizures. Phenytoin is the most important drug in this group, other drugs, ethotoin, mephenytoin, also to treat epilepsy. Prodrugs such as have been created. some cases of trigeminal neuralgia related neuralgia. arrhythmias. Hydantoins or glyc...

The development of new methods for linking sugars to heterocycles and peptides is an attractive area of research because glyco-conjugates play important roles in biology and medicine and are indispensable tools for probing several processes. Herein we report a one-pot, three-component sequential procedure for the synthesis of a novel class of glyco-conjugates, i.e. glyco-hydantoin conjugates, i...

The Red Sea sponge Hemimycale arabica afforded the known (Z)-5-(4-hydroxybenzylidene)-hydantoin (1), (R)-5-(4-hydroxybenzyl)hydantoin (2), and (Z)-5-((6-bromo-1H-indol-3-yl)methylene)-hydantoin (3). The natural phenylmethylene hydantoin (PMH) 1 and the synthetic (Z)-5-(4-(ethylthio)benzylidene)-hydantoin (4) showed potent in vitro anti-growth and anti-invasive properties against PC-3M prostate ...

Synthesis routes to diphenyl hydantoin derivatives in the presence of benzils; 4,4-dimethylbenzil , 4-methylbenzil 4,4-bromobenzil 4-dimethylaminbenzoin and 4-amin-4-nitrobenzoin ure- give condensation benzil urea allowed by benzylic rearrangement.