Prasugrel, a thienopyridine antiplatelet drug, is converted in animals and humans to the pharmacologically active metabolite R-138727 [(2Z)-{1-[(1RS)-2-cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl]-4-sulfanylpiperidin-3-ylidene}ethanoic acid], which has two chiral centers, occurring as a mixture of four isomers. The RS and RR isomers are more active than the SS and SR isomers (RS > RR > > SR = SS)...

Pomalidomide, a potent novel immunomodulatory agent, has been developed as a racemic mixture of its R- and S-isomers. Pharmacokinetic (PK) analyses were conducted to determine the PK disposition of the isomers from their PK profiles in humans and monkeys. Modeling and simulation were performed to describe the observed PK profiles and explore potential differences in isomer disposition and expos...

A procedure for separation/preconcentration of para-aminophenol (PAP) in pharmaceutical formulation, based on cloud point extraction (CPE) as a prior step to determination by UV-Vis spectrophotometry has been developed. The analyte reacted with 4-dimethylamino benzaldehyde (DAB) in acidic media to form a shift base, which were separated and preconcentrated in a mixed micelle of the anionic surf...

Domains of different surface reconstruction – negativelyor positively-buckled isomers – have been previously observed on highly n-doped Si(111)-2×1 surfaces by angle-resolved ultraviolet photoemission spectroscopy and scanning tunneling microscopy/spectroscopy. At low temperature, separate domains of the two isomer types are apparent in the data. It was argued in the prior work that the negativ...

The levels of four pregnanolone isomers and their polar conjugates and pregnenolone sulfate were measured in the plasma of 13 and 7 women at delivery with subarachnoidal and epidural analgesia, respectively, and in corresponding samples of umbilical plasma using a simple quadrupole GC/MS system with electron impact ionization (pregnenolone isomers), RIA following HPLC separation (pregnenolone) ...

A potent plant-derived HIV-1 inhibitor, 3,5-dicaffeoylquinic acid (diCQA), has been shown to undergo isomerisation upon UV exposure where the naturally occurring 3 trans ,5 trans -diCQA isomer gives rise to the 3 cis ,5 trans -diCQA, 3 trans ,5 cis -diCQA, and 3 cis ,5 cis -diCQA isomers. In this study, inhibition of HIV-1 INT by UV-induced isomers was investigated using molecular docking metho...