The Biginelli reaction, which involves the interaction of ethyl acetoacetate, urea, and an appropriate aryl aldehyde, was first discovered by Pietro Biginelli about 120 years ago. The Biginelli products (3,4-dihydropyrimidin-2(1H)-ones) are interesting materials due to their significant pharmacological and structural profiles. In the last decades, the asymmetric synthesis as a powerful tool has an effective impact on the Biginelli products and has increased their potencies and applications as drugs. Having the importance of this subject in mind, in this review we wish to present the recent rapid progress of asymmetric Biginelli reaction.
Background. Attention-deficit hyperactivity disorder (ADHD) is one of the most common psychiatric disorders among children. The aim of this study was to evaluate risk factors for ADHD in children. Method. In this case-control study, 404 children between 4 and 11 years old were selected by cluster sampling method from preschool children (208 patients as cases and 196 controls). All the participants were interviewed by a child and adolescent psychiatrist to survey risk factors of ADHD. Results. Among cases, 59.3% of children were boys and 38.4% were girls, which is different to that in control group with 40.7% boys and 61.6% girls. The chi-square showed statistically significance (P value < 0.0001). The other significant factors by chi-square were fathers' somatic or psychiatric disease (P value < 0.0001), history of trauma and accident during pregnancy (P value = 0.039), abortion proceeds (P value < 0.0001), unintended pregnancy (P value < 0.0001), and history of head trauma (P value < 0.0001). Conclusions. Findings of our study suggest that maternal and paternal adverse events were associated with ADHD symptoms, but breast feeding is a protective factor.
BackgroundA straightforward and efficient method for the synthesis of pyrano[2,3-d]pyrimidine diones derivatives from the reaction of barbituric acid, malononitrile and various aromatic aldehydes using SBA-Pr-SO3H as a nanocatalyst is reported.ResultsReactions proceed with high efficiency under solvent free conditions. Urease inhibitory activity of pyrano[2,3-d]pyrimidine diones derivatives were tested against Jack bean urease using phenol red method. Three compounds of 4a, 4d and 4l were not active in urease inhibition test, but compound 4a displayed slight urease activation properties. Compounds 4b, 4k, 4f, 4e, 4j, 4g and 4c with hydrophobic substitutes on phenyl ring, showed good inhibitory activity (19.45-279.14 μM).DiscussionThe compounds with electron donating group and higher hydrophobic interaction with active site of enzyme prevents hydrolysis of substrate. Electron withdrawing groups such as nitro at different position and meta-methoxy reduced urease inhibitory activity. Substitution of both hydrogen of barbituric acid with methyl group will convert inhibitor to activator.
Indandione is an important starting material that has drawn great attention in various organic transformations because of its attributes, such as low cost, easy to handle and eco-friendliness generally affording the corresponding products in excellent yields. In this review, we summarize recent data describing the most important MCRs reactions in which one of the starting materials is indandione. This review will also present two-, three-, four-, and five-component and one-pot reactions for the functionalization of indandione with the to increase awareness on the versatility of using this compound among organic chemists.
Increased oxidative stress is widely accepted to be a factor in the development and progression of Alzheimer's disease (AD). Here we introduced Salvia sahendica as a protective agent in differentiated PC12 cells, which are commonly considered to be a reliable model of neuronal cells. Our results demonstrated that S. sahendica has antioxidant and antiglycating properties in in vitro system and these properties are expanded into H(2)O(2)-induced model. S. sahendica inhibited H(2)O(2)-induced cell death in PC12 cells. We further showed that this plant exerts its protective effect by increasing superoxide dismutase and catalase levels, reducing lipid peroxidation and upregulating hemoxygenase-1 and glutamylcysteine synthetase proteins. This study raises the possibility of developing S. sahendica as a potential neuroprotective agent.
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