. Orsolini, G. D. Papanti and J. M. Corkery, Novel psychoactive substances of interest for psychiatry, World Psych. 14 (2015) 15–26; https://doi.org/10.1002/wps.20174 5. Y. Boumrah, M. Rosset, Y. Lecompte, S. Bouanani, K. Khimeche and A. Dahmani, Development of a targeted GC/MS screening method and validation of an HPLC/DAD quantification method for piperazines-amphetamines mixtures in seized material, Egypt. J. For. Sci. 4 (2014) 90–99; https://doi.org/10.1016/j.ejfs.2014.03.002 6. C. D. Rosenbaum, S. P. Carreiro and K. M. Babu, Here today, gone tomorrow…and back
RJ. Levamisole receptor phosphorylation: effects of kinase antagonists on membrane potential responses in Ascaris suum suggest that CaM kinase and tyrosine kinase regulate sensitivity to levamisole. J Exp Biol. 2002, 205(24): 3979-3988. 22. Lalchhandama L: Nematocidal effects of piperazine and the extract of Acacia oxyphylla stem bark on the poultry nematode, Ascaridia galli. Pharmacologyonline 2008, 3: 864-869. 23. Tarbiat B: Ascaridia galli in laying hens: Adaptation of a targeted treatment strategy with attention to anthelmintic resistance. Doctoral thesis
In the present study we tested the dose andh time dependence of the antinematodal effects of carvacrol and tyhmol on Caenorabditis elegans, and the efficacy of carvacrol, thymol, p-cymene and cinnamaldehyde,which were administrated in the drinking water of rats naturally infected with the pinworm Syphacia muris. The control treatment of the infected rats was carried out with piperazine. Thymol caused a dose and time-dependent mortality in adult C. elegans. The value of the Median Lethal Concentration (LC50) of thymol was 117.9nM after 24h and 62.89 nM after 48h of exposure. Carvacrol exhibited a higher antinematodal efficiency than thymol. The LC50 of carvacrol, after 24 hours of exposure, was 53.03 nM, while after 48 hours it was 33.83 nM. On the other hand, piperazine showed an extremely high efficacy against S. muris infection in rats. Piperazine, at a dose of 625 mg/kg bw, administered in drinking water continuously for 10 days, eliminates the infection completely. However, none of the investigated active ingredients of essential oils were effective against S. muris. The reason for the lack of efficiency may be due to their pharmacokinetic properties. A relatively low amount of, orally administered, active ingredients of essential oils reaches the distal segments of the gastrointestinal tract, where S. muris inhabits the gut (colon and cecum). The obtained results, on C. elegans, indicate a clear dose and time-dependent antinematodal effect of thymol and carvacrol. However, for clinical application, it is necessary to examine the efficacy of microencapsulated formulations with a controlled release of active ingredients of essential oils in certain parts of the gastrointestinal tract.
Nitroimidazoles. V. Synthesis and anti-HIV evaluation of new 5-substituted piperazinyl-4-nitroimidazole derivatives
A series of 2-alkylthio-1-[4-(1-benzyl-2-ethyl-4-nitro-1H-
-imidazol-5-yl)-piperazin-1-y]lethanones (3-9) and alkyl-
-1-yl)ketones (11-20) as well as the indole analogue 22
were synthesized from 4-nitro-5-piperazinyl imidazole
derivative 1, with the aim to develop newly non-nucleoside
reverse transcriptase inhibitors (NNRTIs). The newly
synthesized compounds were assayed against HIV-1 and
HIV-2 in MT-4 cells. Compound 2 showed inhibition of
HIV-1 (EC50 0.45 mg mL-1) and HIV-2 (0.50 mg mL-1),
while 9 showed inhibition of HIV-1 (EC50 2.48 mg mL-1,
SI = 4).
-oxobenzoxazolidines-3-oxo-2H-1,4-benzoxazines and related compounds. Chem Pharm Bull 1991; 39: 2937-2943. 18. Onkol T, Ito S, Yildirim E, Erol K, Sahin MF. Synthesis and Antinociceptive Activity of (2-Benzazolon-3-yl)propionamide Derivatives. Arch Pharm 2001; 334: 17-20. 19. Mokrosz J, Pietrasiewicz L, Duszynska MM, Marek C. Structureactivity relationship studies of central nervous system (CNS) agents. 5. Effect of the hydrocarbon chain on the affinity of 4-substituted 1-(3-chlorophenyl)piperazines for 5-HT1A receptor sites. J Med Chem 1992; 35: 2369-2374. 20. Gökhan N, Köksal M
Objective: Silver complexes of antibacterial quinolones have the potential advantage of combining the antibacterial activity of silver and fluoroquinolones. The objective of our study was the preparation and the preliminary physico-chemical characterization of a silver complex with ofloxacin.
Methods: To achieve our goals several spectroscopic methods (ultraviolet spectrophotometry, mass spectrometry, and Fourier transform infrared spectroscopy) and thermal methods (differential scanning calorimetry and thermogravimetric analysis) were used in order to elucidate the chemical structure of the complex.
Results: Using mass spectrometry we established the stoichiometric ratio silver:ofloxacin as 1:2. Experimental data suggest a particular coordination for ofloxacin, as a monodentate ligand, in the formation of a complex with silver, through the nitrogen atom from the methyl-piperazine cycle.
Conclusions: The obtained complex has a chemical structure likely [Ag(Ofloxacin)2]NO3, requiring evaluation through other physico-chemical methods.
Observations were made on the intestinal threadworm (Strongyloides westeri) and ascarid (Parascaris equorum) in field studies in 373 Thoroughbred foals on nine farms in Central Kentucky (USA) in 2013. Qualitative examination was made of feces of the foals for presence of S. westeri and P. equorum eggs. The main purpose of the prevalence study was to obtain current data on S. westeri in Thoroughbred foals. This was done to compare these findings with earlier studies in this geographical area where the prevalence of this parasite has been very low the last several decades. All the foals except on one farm had been treated one or more times with a parasiticide before the study. Prevalence of S. westeri in foals was 0 to 3 % on two farms, 6 to 9 % on three farms, and 20 to 51 % on four farms. The prevalence of P. equorum in foals was 0 to 14 % on three farms, 27 to 38 % on three farms, and 46 to 51 % on three farms. Effect of drugs given before the current study, on the prevalence of the two parasitic nematode species, is discussed. Also, three field tests were done by the present authors to evaluate activity of three individual or combination of drugs against ascarids. Evaluation was somewhat limited because, on two of the farms, a relatively small number of foals was passing ascarid eggs before treatment. However, oxibendazole and oxibendazole/piperazine combination were much more efficacious than fenbendazole.
Synthesis and anthelmintic activity of some novel 2-substituted-4,5-diphenyl imidazoles
A series of 2-substituted-4,5-diphenyl imidazoles 1a-j were synthesized by refluxing benzil with different substituted aldehydes in the presence of ammonium acetate and glacial acetic acid. Structures of the synthesized compounds were confirmed on the basis of IR, 1H NMR and mass spectral data. Compounds 1a-j were screened for anthelmintic activity. Test results revealed that compounds showed paralysis time of 0.24 to 1.54 min and death time of 0.39 to 4.40 min while the standard drugs albendazole and piperazine citrate showed paralysis time of 0.54 and 0.58 min and death time of 2.16 and 2.47 min, respectively, at the same concentration of 1% (m/V). Five compounds, 2-[2-hydroxyphenyl]-4,5-diphenyl imidazole (1b), 2-[3-methoxyphenyl]-4,5-diphenyl imidazole (1c), 2-[2-phenylethenyl]-4,5-diphenyl imidazole (1e), 2-[4-fluorophenyl]-4,5-diphenyl imidazole (1g) and 2-[3-nitrophenyl]-4,5-diphenyl imidazole (1h) showed significant anthelmintic activity compared to the standard drugs.
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