The Behavior of 3,3-Diphenylindan-1,2-dione Towards Alkyl Phosphites

The reaction of 3,3-diphenylindan-1,2-dione with trimethyl phosphite in dry benzene at room temperature for about 15 h led to the formation of a mixture containing dimethyl (3,3-diphenyl-2-methoxy-1-indenyl)phosphate and dimethyl (3,3-diphenyl-1H-2-oxo-1-indanyl)phosphate, whereas with triisopropyl phosphite, diisopropyl (3,3-diphenyl-2-isopropoxy-1-indenyl)phosphate is the only product. Treatment of the dione with dialkyl phosphites under different experimental conditions gave dialkyl (3,3-diphenyl-1-hydroxy-2-oxo-1-indanyl)phosphates. Reaction mechanisms are presented which account for the experimental results. Structural assignments of the new compounds are based on the spectroscopic evidences and two examples were elucidated by X-ray crystallography.     

Bioactive compounds and antioxidant activity of Rhaponticum acaule (L.) DC

Abstract

Rhaponticum acaule (L.) DC. is a medicinal plant commonly used for the treatment of some illnesses such as gastrointestinal infections. In this work, we report the composition of different parts of this plant on phenolic compounds, their quantification, and antioxidant activity. The obtained results reported that methanolic extracts of the three parts studied revealed high phenolic contents. For flavonoid contents, the highest contents were reported in organic extracts of leaf part. In addition, results obtained from the study of the antioxidant activity showed that methanolic extract of root presented the highest activity, in DPPH^? scavenging ability test with an IC₅₀ of 0.31?±?0.04?mg/mL and in FRAP test with an EC₅₀ of 1.06?±?0.02?mg/mL. The RP-HPLC-PDA analysis revealed the presence of five phenolic acids (sinapic, caffeic, chlorogenic, ferulic and syringic acids), one flavanone (naringenin), one flavonol (rutin) and vanillin.     

Determination of some polycyclic aromatic hydrocarbons in filter tar of Turkish cigarettes

A simultaneous determination method for the analysis of benzo[a]pyrene (BaP) and dibenzo[a,h]anthracene (DahA) in the filter tar of Turkish cigarettes has been developed. The method involved (a) the extraction of BaP and DahA with n-hexane from ACN solution in which the cigarette filters were extracted, and then (b) purification of the n-hexane extracts by elution on an XAD-2 column using n-hexane/dichloromethane (9:1, v/v) mixture. Separation and quantitative determination of BaP and DahA in the extracts were carried out by HPLC and fluorescence detection on a C18 RP column. The calculated recoveries for BaP and DahA were found in the range of 90-100% for each extraction and clean-up steps. Analysis of various filter tar of Turkish cigarettes showed that an average of 74.28 ng/filter of BaP and 5.24 ng/filter of DahA were present in Turkish cigarettes.     

Minecosid und Verminosid,zwei neue Iridoidglucoside aus Veronica officinalisL. (Scrophulariaceae)

Minecoside and verminoside, two new iridoid glucosides from Veronica officinalis L. (Scrophulariaceae) Two new esters of catalpol, minecoside ( 1 ) and verminoside ( 3 ), have been isolated from Veronica officinalis L. The structures of 1 and 3 have been determined on the basis of the spectral data as 6-isoferuloylcatalpol and 6-caffeeoylcatalpol, respectively.     

Determination of 1,4-benzodiazepines in drug dosage forms by difference spectrophotometry

A spectrophotometric method has been developed for the determination of seven 1,4-benzodiazepines, namely: chlordiazepoxide, diazepam, nitrazepam, oxazepam, lorazepam, temazepam and cinolazepam. The method involves reduction of the target compounds using Zn/HCl and measuring the difference in the absorbance before and after reduction. The quantities of zinc and acid required for efficient reduction were carefully studied. 1–20 g ml^–1 of the compounds could be determined with < 1% error. The method was applied successfully to the determination of these compounds in pharmaceutical dosage forms. The results were sufficiently accurate and precise and comparable to those from the official methods.     

Polarographic and spectrophotometric determination of isocarboxazid and tranylcypromine sulphate through treatment with nitrous acid

Two methods are described for the determination of two widely prescribed antidepressants, namely isocarboxazid and tranylcypromine sulphate as the pure drugs and in dosage forms. Both methods involve prior treatment with nitrous acid. In the Spectrophotometric method, the two derivatives obey Beer's law over the concentration range 1–20 g/ml. The derivatives are polarographically reducible withE _1/2 values of –0.84 and –0.73 V for isocarboxazid and tranylcypromine sulphate, respectively. The calibration plots are linear over the range 4.3 × 10^–5–3.0 × 10^–4 and 1.1 × 10^–5–1.65 × 10^–4 mol/1 for isocarboxazid and tranylcypromine sulphate, respectively. The results obtained for assays for the two drugs compare satisfactorily with those given by the official methods.     

HPLC Quantification of Vitexine-2″-O-rhamnoside and Hyperoside in Three Crataegus Species and Their Antimicrobial and Antiviral Activities

Crataegus sp., also known as “hawthorn”, is one of the most prescribed herbal drugs and approved to be used against congestive heart failure. The extract is required to be standardized according to its flavonoid (vitexine-2″-O-rhamnoside and hyperoside) and oligomeric procyanidin content by the European Pharmacopoeia (EP). In this study, the leaves and berries of three Crataegus species including C. aronia var. aronia, C. monogyna ssp. monogyna (from two different localities) as well as C. pseudoheterophylla growing in Turkey were evaluated for their vitexine-2″-O-rhamnoside and hyperoside content by reversed-phase HPLC as well as their total procyanidin amount by a spectrophotometric method. In addition, antibacterial, antifungal, and antiviral activities of the extracts were also determined. Our results indicated that C. monogyna ssp. monogyna samples of both localities met the criteria required by the EP for their total flavonoid amount (2.49 and 2.86%) and total proanthocyanidin content (1.56 and 2.22%). According to data we obtained, the extracts have been verified to be highly effective against Candida albicans and Herpes simplex virus.

     

Green preparation of Pd nanoparticles on SBA-15 via supercritical fluid deposition and application on Suzuki–Miyaura cross-coupling reaction

A well-dispersed green Pd/SBA-15 catalyst with an average size of 13.7 nm and 492.6 m²/g BET surface area is prepared via supercritical fluid deposition method with a new bipyridyl precursor that enables reduction at mild conditions at 80 °C and 17.2 MPa. The catalytic performance of Pd/SBA-15 prepared using scCO₂ with hydrogen reduction was assessed for Suzuki–Miyaura coupling reaction of bromobenzene and phenylboronic acid that was chosen as a model coupling reaction. The catalyst was tested in six different solutions and in three organic and inorganic bases during reactions. In general, the effect of bases is investigated when solvents are held constant and K₂CO₃ appears to have the best results in the activity studies used. For each of the 3 bases used, the highest catalytic activity was reached as the result of the solvent system being ethanol/water (1:1). The highest catalytic conversion was obtained in the ethanol-K₂CO₃ solvent-base pair. The catalyst synthesized in this study exhibited high activities and TON value was found as 160.8 at room temperature.     

Design,Synthesis, and Pharmacological Assay of Novel Compounds Based on Pyridazine Moiety as Potential Antitumor Agents

In an endeavor to develop antitumor agents, we made a credible survey regarding synthesis, structure, and pharmacological assay of novel pyridazine derivatives, so that 2‐((6‐(4‐chloro‐3‐methylphenyl)pyridazin‐3‐yl)oxy)acetohydrazide 3 was utilized as scaffold to build novel compounds 4 – 19 by reaction with various electrophilic reagents, followed by determination and explanation atropisomerism phenomena and tauomerism ratio such as keto‐enol and lactam–lactim tautomers for some synthesized compounds. In vitro, these compounds were screened for antitumor efficacy versus two cell lines, namely, hepatocellular carcinoma and mammary gland breast cancer, by using MTT assay. Among the examined compounds, compound 16 was exhibited promising potent activity (IC₅₀ = 8.67 ± 0.7 μM) versus HepG2 cell line. Meanwhile, compounds 3 and 16 were manifested the very highest efficacy (IC₅₀ = 5.68 ± 0.6 and 9.41 ± 0.9 μM) versus MCF‐7 cell line.