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Annual Reports in Medicinal Chemistry continues to focus on providing timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expected to provide the basis for entirely new future therapies. Sections I-IV are disease orientated and generally report on specific medicinal agents. Sections V and VI continue to emphasize important topics in medicinal chemistry, biology, and drug design. Annual comprehensive reviews of the past year literature in many topics of interest to medicinal chemistsIncludes a comprehensive set of indices to easily locate topics in Volumes of this seriesProvides critical review on hot topics in medicinal chemistry.

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Annual Reports in Medicinal Chemistry

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    I appreciate your efforts in excellence for organizing Food Technology Furthermore, novel synthetic and semisynthetic derivatives of DIC, as potential antitumor agents, have gained increasing attention in medicinal research [ 11 ]. Our previous studies have demonstrated that DIC is a promising drug candidate with favorable oral pharmacokinetic profiles [ 12 , 13 ].

    Kundrecensioner

    Very recently, using in vitro microsomal incubation systems, we systematically studied the metabolites of DIC in human and animal liver microsomal incubation systems [ 14 ], and we found that the metabolic fate of DIC in human liver microsomes was about the same as that in mouse liver microsomes, while with some differences compared with that in rat, dog, and monkey liver microsomes.

    We elucidated that the o-demethylation, monohydroxylation, N -oxidation, and 2,3-olefinic epoxidation pathways are the major metabolic routes of DIC [ 14 ].


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    In a separate study [ 15 ], a N -acetylcysteine NAC conjugate which was derived from the reactive DIC metabolite, 2,3-epoxide DIC, was detected in the rat liver microsomal incubation system, as well as in DIC-treated rat urine samples. It is also remarkable to note that there are no reports about the in vivo metabolism study of DIC in either humans or mice. Choosing the most relevant animal species to conduct studies is essential for researchers to extrapolate results from studies performed in animals onto human [ 16 — 19 ].

    Annual reports in medicinal chemistry Abbreviation | ISSN - Journal Abbreviation Database

    In the preset study, based on the previous results [ 14 , 15 ], the in vivo metabolism study of DIC was performed on mice. A powerful hybrid linear quadrupole ion trap orbitrap LTQ-Orbitrap mass spectrometer equipped with a high-performance liquid chromatography HPLC system was used for the structural elucidation of the metabolites.

    Mice were allowed to acclimate for at least 1 week prior to the start of the experiment. Mice were fed with AIN semipurified diet and were allowed ad libitum food and water throughout the study. Metabolic cages were used for the collection of twenty-four-hour mouse urine and fecal samples. The urine and plasma samples were deconjugated by the enzyme as described previously with slight modifications [ 20 , 21 ].

    Annual Reports in Medicinal Chemistry Volume 43

    Three healthy volunteers mean age, For the in vitro fermentation experiment, a pooled human stool slurry was made by direct mixing of an equal volume of the stool slurry from each subject. A Phenomenex Gemini C18 column 3.

    Annual Reports in Medicinal Chemistry: Platform Technologies in Drug Discovery and Validation

    The HPLC conditions were the same as we described before [ 14 ]. The flow rate was set at 0. Nitrogen was used as a sheath and auxiliary gas with 30 and 10 arbitrary units, respectively, and helium was applied as the collision gas. Collision-induced dissociation CID energy was set at 35 for MS n analysis with an isolation width set at 1. Data acquisition and analysis were performed using Xcalibur software 2.