Novel Synthesis of N‐Methyl Spiropyrrolidines by 1,3‐Dipolar Cycloaddition Reaction of Azomethine Ylides

A series of novel N‐methyl spiropyrrolidines have been synthesized in good yield by the cycloaddition reaction of azomethine ylides generated by a decarboxylative route from sarcosine and paraformaldehyde with conformationally locked s‐trans enone functionality present in the (E)‐3‐arylidene‐4‐chromanone as dipolarophiles. The structure of the title compound was established by spectroscopic techniques.     

Rapid identification and quantification of chlorpheniramine maleate or pheniramine maleate in pharmaceutical preparations by thin-layer chromatography-densitometry

Thin-layer chromatography (TLC)-densitometry was used to separate, identify, and quantitate chlorpheniramine maleate (CPM) and pheniramine maleate (PM) when present in combination with other drugs in pharmaceutical preparations of tablets, syrups, eye and ear drops, etc. CPM or PM was extracted (tablets, capsules, etc.) or diluted (liquid preparations, if needed) with 80% ethanol and isolated from other ingredients by TLC on silica gel G using cyclohexane-chloroform-methanol-diethylamine (4.5 + 4.0 + 0.5 + 1.0, v/v) as the mobile phase. Separated CPM and PM were detected under shortwave ultraviolet light and quantitated by scanning densitometry at 260 nm. Recoveries of CPM and PM were 100.09+/-0.77% and 100.09+/-0.87%, respectively.     

Kinetics and mechanism of oxidation of N,α-diphenylnitrones by 4-(dimethylamino)pyridinium chlorochromate (DMAPCC) in aqueous DMF medium

The kinetics of oxidation of aldonitrones by 4-(dimethylamino)pyridinium chlorochromate (DMAPCC) has been studied in aqueous N,N-dimethylformamide in the presence of perchloric acid. The reaction follows first-order kinetics with respect to each of DMAPCC and nitrone. The order with respect to [H⁺] was found to be close to zero. The rate of oxidation was unaltered by the variation of [NaClO₄] but addition of MnSO₄ decreased the rate. The reaction rate was found to decrease with a decrease in dielectric constant of the medium. Electron-releasing and electron-withdrawing groups perturb the reaction rate with a good Hammett correlation. The oxidation products were found to be benzaldehyde and nitrosobenzene. The reaction was carried out at four different temperatures and the activation parameters have been calculated. On the basis of the experimental findings, a suitable mechanism has been proposed.     

Crystal structure and DFT analyses of a pentacoordinated PCP pincer nickel(II) complex

The reaction of NiCl₂ with 1,3‐bis[(diphenylphosphanyl)methyl]hexahydropyrimidine in the presence of 2,6‐dimethylphenyl isocyanide and KPF₆ afforded a new pentacoordinated PCP pincer Ni^II complex, namely {1,3‐bis[(diphenylphosphanyl)methyl]hexahydropyrimidin‐2‐yl‐κN²}(2,6‐dimethylphenyl isocyanide‐κC)nickel(II) hexafluoridophosphate 0.70‐hydrate, [Ni(C₉H₉N)(C₃₀H₃₀ClN₂P₂)]PF₆·0.7H₂O or [NiCl{C(NCH₂PPh₂)₂(CH₂)₃‐κ³P,C,P′}(Xylyl‐NC)]PF₆·0.7H₂O, in very good yield. Its X‐ray structure showed a distorted square‐pyramidal geometry and the compound does not undergo dissociation in solution, as shown by variable‐temperature NMR and UV–Vis studies. Density functional theory (DFT) calculations provided an insight into the bonding; the nickel dsp²‐hybridized orbitals form the basal plane and the nearly pure p orbital forms the axial bond. This is consistent with the NBO (natural bond orbital) analysis of analogous nickel(II) complexes.     

Synthesis of trans-Disubstituted Alkenes by Cobalt-Catalyzed Reductive Coupling of Terminal Alkynes with Activated Alkenes

A cobalt-catalyzed reductive coupling of terminal alkynes, RC?CH, with activated alkenes, R'CH?CH(2) , in the presence of zinc and water to give functionalized trans-disubstituted alkenes, RCH?CHCH(2) CH(2) R', is described. A variety of aromatic terminal alkynes underwent reductive coupling with activated alkenes including enones, acrylates, acrylonitrile, and vinyl sulfones in the presence of a CoCl(2) /P(OMe)(3) /Zn catalyst system to afford 1,2-trans-disubstituted alkenes with high regio- and stereoselectivity. Similarly, aliphatic terminal alkynes also efficiently participated in the coupling reaction with acrylates, enones, and vinyl sulfone, in the presence of the CoCl(2) /P(OPh)(3) /Zn system providing a mixture of 1,2-trans- and 1,1-disubstituted functionalized terminal alkene products in high yields. The scope of the reaction was also extended by the coupling of 1,3-enynes and acetylene gas with alkenes. Furthermore, a phosphine-free cobalt-catalyzed reductive coupling of terminal alkynes with enones, affording 1,2-trans-disubstituted alkenes as the major products in a high regioisomeric ratio, is demonstrated. In the reactions, less expensive and air-stable cobalt complexes, a mild reducing agent (Zn) and a simple hydrogen source (water) were used. A possible reaction mechanism involving a cobaltacyclopentene as the key intermediate is proposed.     

A Comparative Study of Biologically and Chemically Fabricated Synthesized AgNPs’ Supplementation with Respect to Heat-Shock Proteins,Survival, and Hatching Rates of Chicken Embryos: An In Ovo Study

The present study examined the characterization and concentration of Brassica oleracea L. var. capitata f. rubra (BOL, commonly known as red cabbage) extracted AgNPs (BOL-AgNPs) and chemically (CHE) synthesized AgNPs (CHE-AgNPs) in chicken embryos through in ovo injections. We investigated the effects of both AgNPs on the survival, hatchability, body weight, and expressions of heat-shock proteins (HSPs). The BOL-AgNPs and CHE-AgNPs at (T1) amounted 100, at (T2) 1000, at (T3) 2500, and at (T4) 5000 µg/100 µl/egg, respectively through in ovo injections. At the end of the experimental period, the body and liver weights of the chicks were altered between the groups and among the concentrations. The serum levels of SGOT and SGPT were significantly increased at BOL-T3 and -T4. Survival and hatching rates were more reduced in the BOL-T3- and -T4-treated groups than at BOL-T1 and -T2. Nevertheless, they were more diminished in the CHE-AgNPs than in the BOL-AgNPs. The CHE-AgNPs revealed the presence of micronuclei and nuclear abnormalities, in contrast to BOL-T4. The mRNA and protein expressions of HSP-60 and 70 in the liver were higher in CHE-AgNPs than in BOL-AgNPs. Hence, plant-synthesized AgNPs are superior in ovo nano-nutrition carriers of nutrients without toxicity than CHE-AgNPs.     

Synthesis and structural characterization of chiral dicationic imidazolophanes

Various chiral dicationic benzimidazolophanes were obtained from optically pure (S)-BINOL, benzimidazole and a suitable aryl alkyl dibromide.     

Tilianin: A Potential Natural Lead Molecule for New Drug Design and Development for the Treatment of Cardiovascular Disorders

Cardiovascular disorders (CVDs) are the leading risk factor for death worldwide, and research into the processes and treatment regimens has received a lot of attention. Tilianin is a flavonoid glycoside that can be found in a wide range of medicinal plants and is most commonly obtained from Dracocephalum moldavica. Due to its extensive range of biological actions, it has become a well-known molecule in recent years. In particular, numerous studies have shown that tilianin has cardioprotective properties against CVDs. Hence, this review summarises tilianin’s preclinical research in CVDs, as well as its mechanism of action and opportunities in future drug development. The physicochemical and drug-likeness properties, as well as the toxicity profile, were also highlighted. Tilianin can be a natural lead molecule in the therapy of CVDs such as coronary heart disease, angina pectoris, hypertension, and myocardial ischemia, according to scientific evidence. Free radical scavenging, inflammation control, mitochondrial function regulation, and related signalling pathways are all thought to play a role in tilianin’s cardioprotective actions. Finally, we discuss tilianin-derived compounds, as well as the limitations and opportunities of using tilianin as a lead molecule in drug development for CVDs. Overall, the scientific evidence presented in this review supports that tilianin and its derivatives could be used as a lead molecule in CVD drug development initiatives.     

Existence results for impulsive neutral evolution integrodifferential equations with infinite delay

In this paper we prove the existence of mild solutions for impulsive neutral evolution integrodifferential equations with infinite delay in Banach spaces. The results are obtained by using the analytic semigroup theory and the Krasnoselski–Schaefer type fixed point theorem. An example is provided to illustrate the theory.