The molecular diversity scope of 1,3-indandione in organic synthesis.

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.

Recent progress in asymmetric Biginelli reaction.

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.

Three-component synthesis of pyrano[2,3-d]-pyrimidine dione derivatives facilitated by sulfonic acid nanoporous silica (SBA-Pr-SO3H) and their docking and urease inhibitory activity.

BACKGROUND: A 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. RESULTS: Reactions 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). DISCUSSION: The 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.

Comparison of the outcomes of normal vaginal delivery with and without spinal anesthesia in mothers admitted to the maternity ward of Firoozabadi Hospital.

Introduction and Objective: The study of the methods of controlling labor pain is very important. One of the methods of pain relief is spinal anesthesia. Due to the different opinions about the effects of spinal anesthesia on the delivery process and maternal and fetal consequences, this study aimed to evaluate the effects of spinal anesthesia and compare it with normal vaginal delivery without spinal anesthesia. Methods: In this retrospective cohort study, 120 mothers, who were admitted to the maternity ward of Firoozabadi Hospital for delivery, were examined. The patients who met the inclusion criteria were divided into two groups of 60 people, one group receiving spinal anesthesia and one without spinal anesthesia, and then, were evaluated in terms of clinical variables and complications of the mother and fetus. Data were analyzed using SPSS statistical software. Results: The mean age of the mothers was 26.6 ± 5.9 years. Five mothers (4.2%) who received spinal anesthesia underwent emergency cesarean section and a significant difference was shown between the two groups (P = 0.02). The mean duration of the active phase of labor did not show a statistically significant difference between the two groups (P = 0.2), but the duration of the second phase of labor was significantly longer in the mothers who received spinal anesthesia (P = 0.008). Conclusion: Spinal anesthesia can be used as a low-complication method in vaginal delivery to reduce pain.

Synthesis of Some Spiro Indeno[1,2-b]pyrido[2,3-d]Pyrimidine-5,3'-Indolines as New Urease Inhibitors.

New series of spiro indeno[1,2-b]pyrido[2,3-d]pyrimidine-5,3'-indolines as new urease inhibitors were synthesized by the catalytic procedure in high yield and short reaction time. In this method, biacidic carbon was prepared as a novel heterogeneous acid and was subsequently used as an efficient catalyst. The inhibitory activities of synthesized compounds were tested against Jack bean urease using Berthelot colorimetric assay and docking simulation using AutoDock 4.2. The compound 4a with IC50 =1.94 µM has the most inhibitor activity in this study. Other derivatives such as 4b, 4d, 4e and 7a were found to be more potent urease inhibitors than the standard inhibitor hydroxyurea, yielding IC50 values of 4.35, 5.557, 7.44, 2.81 and 14.46 µM, respectively (IC50 of hydroxyurea = 100 µM).

Green Synthesis and Urease Inhibitory Activity of Spiro-Pyrimidinethiones/Spiro-Pyrimidinones-Barbituric Acid Derivatives.

Sulfonic acid functionalized SBA-15 (SBA-Pr-SO3H) with pore size 6 nm as an efficient heterogeneous nanoporous solid acid catalyst exhibited good catalytic activity in the Biginelli-like reaction in the synthesis of spiroheterobicyclic rings with good yield and good recyclability. Spiro-pyrimidinethiones/spiro-pyrimidinones-barbituric acid derivatives were synthesized in a simple and efficient method using the one-pot three-component reaction of a cyclic 1,3- dicarbonyl compounds (barbituric acid), an aromatic aldehyde and urea or thiourea in the presence of nanoporous silica SBA-Pr-SO3H under solvent free conditions. Urease inhibitory activity of spiro compounds were tested against Jack bean urease using Berthelot alkaline phenol-hypochlorite method. Five of 13 compounds were inhibitor and two of them were enzyme activators. Analysis of the docking results showed that, in most of the spiro molecules, one of the carbonyl groups is coordinated with both nickel atoms, while the other one is involved in the formation of hydrogen bonds with important active-site residues. The effect of inserting two methyl groups on N atoms of barbiturate ring, S substituted, ortho, meta and para substituted compounds were investigated too.

Evaluation of attention-deficit hyperactivity disorder risk factors.

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.