Rümeysa Demirdamar

Synthesis and antidepressant evaluation of new 3-phenyl-5-sulfonamidoindole derivatives

Abstract Ten new arylidenehydrazides were synthesized by reacting 3-phenyl-5-sulfonamidoindol-2-carboxylic acid hydrazide with various aldehydes and a new N 2 -substituted hydrazide was prepared by reduction of 3-phenyl-5-sulfonamidoindole-2-carboxylic acid benzylidene-hydrazide 2 with sodium borohydride. The chemical structures of the compounds were verified by means of their IR, 1 H-NMR, El mass spectroscopic data and elemental analyses. The antidepressant activity of these compounds were evaluated by the Porsolt forced swimming (behavioral despair) test using tranylcypromine as the standard. 3-Phenyl-5-sulfonamidoindole-2-carboxylic acid 3,4-methylenedioxybenzylidenehydrazide, 3-phenyl-5-sulfonamidoindole-2-carboxylic acid 4-methylbenzylidenehydrazide, 3-phenyl-5-sulfonamidoindole-2-carboxylic acid 4-nitrobenzylidenehydrazide and 3-phenyl-5-sulfonamidoindole-2-carboxylic acid benzylidenehydrazide showed antidepressant activity at 100 mg/kg.

Reactive oxygen species-induced impairment of endothelium-dependent relaxation in rat aortic rings: protection by L-arginine.

The protective effect of L-arginine against reactive oxygen species-induced impairment of endothelium-dependent vasorelaxation was investigated in isolated ring preparations of rat aorta. The aortic rings were subjected to reactive oxygen species generated by the electrolysis of the bathing solution or incubation with H2O2. Endothelium-dependent relaxation in response to acetylcholine of precontracted aortic rings was attenuated when the rings were exposed to reactive oxygen species or H2O2. Incubation prior to electrolysis with either L-arginine, the endogenous precursor of nitric oxide (NO), or sodium nitroprusside, an exogenous donor of NO, protected the aortic rings against the impairment of endothelium-dependent relaxation. However, D-arginine and glycine, amino acids which do not produce NO, also afforded protection in this model. Therefore, not only the increased synthesis of NO but also the oxidation of L-arginine, with concomitant disproportionation of reactive oxygen species, may be responsible for the protective effect against reactive oxygen species-induced loss of the endothelial response to acetylcholine in isolated rat aorta.

Condensed Heterocyclic Compounds: Synthesis and Antiinflammatory Activity of Novel Thiazolo[3,2-a]pyrimidines

In this study, thirty six new 2‐benzylidene‐7‐methyl‐3‐oxo‐5‐phenyl‐2,3‐dihydro‐5H‐thiazolo[3,2‐a]pyrimidine‐6‐carboxylic acid methyl esters were synthesized and characterized by spectral, crystallographic, and elemental analysis. The antiinflammatory activity of the compounds was tested by the carrageenan hind paw edema test. It was found that compound 6a having a 2‐methoxyphenyl group at position 5 and a benzylidene group at position 2 was the most potent compound in this series. All the compounds that were tested for ulcer activity gave positive results.

The Knowledge and Attitude of the Healthcare Professionals towards Pharmacovigilance and Adverse Drug Reaction Reporting in NorthernCyprus

Background: Adverse drug reaction (ADR) is a response to a medicinal product which is noxious and unintended. Spontaneous reporting of ADRs has remained the cornerstone of pharmacovigilance and is important in maintaining patient safety. Therefore, we aimed to assess knowledge and attitude of the health professionals towards pharmacovigilance and ADR reporting. Method: A face to face questionnaire was conducted with 90 community pharmacists, 98 nurses and 71 physicians in Turkish Republic of Northern Cyprus (TRNC), who consented to participate in the study. Results: Of those that did respond, only 13% of the pharmacists, 2% of the nurses and 20% of the physicians had knowledge about ‘pharmacovigilance’. Respectively 32%, 12% and 54% of participants stated that their patients reported them an ADR within the recent year, but only 10% of the pharmacists and 3% of nurses and physicians stated that they sent an ADR report to the concerned organization. The common reasons for under-reporting was stated as lack of knowledge of where/how to report, lack of time, ADR reporting being not mandatory, belief that it was not their responsibility, hesitation about their clinical knowledge, avoiding the professional liability. Conclusion: The results show that the healthcare professionals in Northern Cyprus have insufficient knowledge about pharmacovigilance. Therefore, it seems there is an extensive need for a training program about pharmacovigilance and ADR reporting.

Analgesic activity of acylated 2-benzoxazolinone derivatives

Ten new benzoxazolinone derivatives having a disubstituted benzoyl group at the six position of the ring were synthesized by reacting 2-benzoxazolinone with aromatic carboxylic acids in the presence of polyphosphoric acid. The structure of the compounds were elucidated by IR, 1H NMR, MS and elemental analysis. Analgesic activity was evaluated by a modified Koster test. Seven compounds showed analgesic activities higher than that of acetylsalicylic acid.

Synthesis of some novel oxime ether derivatives and their activity in the 'behavioral despair test'

Abstract In this study, a new series of 2-aminoethyloxime ether derivatives of some aralkylketones was synthesized. Their structures have been elucidated by UV, IR, 1 H-NMR, 13 C-NMR, mass spectra and elementary analysis. These compounds were then screened for their inhibition of immobility as an indicator of possible antidepressant activities by using the ‘behavioral despair test’. Results showed that all the new compounds decreased the immobility time, however, the inhibition observed with AO3 , AO4 and HO1 was significantly higher compared to fluvoxamine ( p

Novel Antiinflammatory Analgesics: 3-(2-/4-Pyridylethyl)-Benzoxazolinone and Oxazolo[4,5-β]pyridin-2-one Derivatives

Twenty‐two new 3‐[2‐(2‐and/or 4‐pyridyl)ethyl]benzoxazolinone and oxazolo[4,5‐b]pyridin‐2‐one derivatives have been synthesized by reacting 2‐and/or 4‐vinylpyridine and appropriate benzoxazolinones and oxazolo[4,5‐b]pyridine‐2‐one. Their chemical structures have been proven by IR, 1H‐NMR, 13C‐NMR, mass spectroscopy, and elemental analysis. The analgesic activities of these compounds were investigated by a modified Koster′s Test. Test results revealed that, at 100 mg/kg dose level, most of the compounds showed significant analgesic activities when compared to aspirin. Therefore the compounds were screened for their antiinflammatory activities using the carrageenan hind paw edema test. Compounds 1, 7, 10, 11, 12, 13, 15, 18, 20, 21 were found more active than indomethacine. In gastric ulceration studies gastrointestinal bleeding was not observed at 100 mg/kg dose level in compounds 1 and 2.

The evaluation of prescription dispensing scores of the pharmacy students before and after the problem-based “rational drug use” course: Results of the two years’ experience

Eczacilarin ilaclarin akilci kullaniminin saglanmasindaki onemi buyuktur. Bu nedenle eczacilik fakulterindeki egitimin farmakoterapi surecinde problem cozme ve karar verme yetilerini kazandiracak nitelikte olmasi gerekir. Probleme dayali yontemlerle yapilan egitim ogrencinin edindigi teorik bilgiyi uygulamada kullanma becerisini kazanmasina yardimci olabilir. Bu calismada Yakin Dogu Universitesi Eczacilik Fakultesi’nde 3. Sinif ogrencileri icin 2011 ve 2012 yillarinda acilan “Akilci Ilac Kullanimi” dersinin recete karsilama skoruna etkisi Turk Farmakoloji Dernegi tarafindan gelistirilen OSPE degerlendirme olcegi ile arastirilmistir. Ogrencilerin derse baslamadan onceki recete karsilama skoru A grubundaki 34 ogrenci icin 34.26 ± 13.6 ve B grubundaki 17 ogrenci icin 34.94 ± 11.6 iken bu degerler kurs bitiminde yapilan degerlendirmede anlamli olarak (p<0.001) artmis; sirasiyla 62.18 ± 13.0 ve 67.06 ± 15.6’a cikmistir. Simule hasta kullanilarak probleme dayali yontemle yapilan farmakoterapi dersleri recete karsilama davranisinin iyilestirilmesi acisindan yararli gozukmektedir