Pyrroloquinone ring systems are important structural units present in many biologically active molecules including a number of marine alkaloids. For example, they are found in a series of marine metabolites, such as tsitsikammamines, zyzzyanones, wakayin, and terreusinone. Several of these alkaloids have exhibited antimicrobial, antimalarial, antifungal, antitumor, and photoprotecting activitie...

Glyoxal and methylglyoxal are reactive dicarbonyl metabolites formed and metabolized in physiological systems. Increased exposure to these dicarbonyls is linked to mutagenesis and cytotoxicity and enhanced dicarbonyl metabolism by overexpression of glyoxalase 1 is linked to tumour multidrug resistance in cancer chemotherapy. We report herein that glycation of DNA by glyoxal and methylglyoxal pr...

The reaction of cyanothioacetamide with aromatic aldehydes and 1,3-dicarbonyl compounds followed by aminomethylation or S-alkylation gave a series heterocyclic derivatives 1,2,3,4-tetrahydropyridine 1,4,5,6,7,8-hexahydroquinoline fragment. resulting were tested for analgesic activity in vivo. Some the prepared showed an antinociceptive effect superior to that ketorolac dynamics.

We have previously shown that 2-acetylcyclopentanone (2-ACP), an enolate-forming 1,3-dicarbonyl compound, provides protection in cell culture and animal models of oxidative stress. The pathophysiology of ischemia-reperfusion injury (IRI) involves oxidative stress, and, therefore, we determined the ability of 2-ACP to prevent this injury in a rat liver model. IRI was induced by clamping the port...

The primary role of yeast Ara1, previously mis-annotated as a D-arabinose dehydrogenase, is to catalyze the reduction of a variety of toxic α,β-dicarbonyl compounds using NADPH as a cofactor at physiological pH levels. Here, crystal structures of Ara1 in apo and NADPH-complexed forms are presented at 2.10 and 2.00 Å resolution, respectively. Ara1 exists as a homodimer, each subunit of which ado...

Highly functionalized multisubstituted 1,4-dihydropyridines 5 have been concisely synthesized in moderate to good yields via L-proline-catalyzed one-pot multicomponent reactions (MCRs) of alkynoates or alkynones 1, amines 2, beta-dicarbonyl compounds 3 and aldehydes 4 under mild conditions. The MCR process involves hydroamination/Knoevenagel condensation/Michael-type addition/intramolecular cyc...

1,1 0-Ferrocene dicarboxylic acid pyridin-4-yl ester (1) is prepared from 1,1 0-ferrocene dicarbonyl chloride and 4-hydroxypyridine. This new bidentate ferrocenoyl ligand reacts with the monocationic complex [(g-p-cymene)2Ru2(l-OH)3] + to give the dicationic complex [(g-p-cymene)2Ru2(l-OH)2(1,1 0(NC5H4–OOC)2–Fc)] 2+ (2) (Fc: C5H4–Fe–C5H4), isolated as a tetrafluoroborate salt. The single-crysta...

the tumors in which odontogenic differentiation is fully expressed are the odontomas. odontomas are considered as hamartomas rather than a true neoplasm. these tumors are composed of enamel, dentine, cementum and pulp tissue. it is most commonly associated with the eruption of the teeth. they are usually discovered on routine radiographic examination. in exceptional cases, the odontoma erupts i...