Zeynep Maraş Özdemir

Synthesis, Anticonvulsant and Antimicrobial Activities of Some New [1-(2-Naphthyl)-2-(pyrazol-1-yl)ethanone]oxime Ethers

In this study, 12 new oxime ether derivatives, which were expected to show anticonvulsant and antimicrobial activities, were synthesized. Oxime ether derivatives were synthesized by the reaction of various alkyl halides with 1-(2- naphthyl)-2-(pyrazol-1-yl)ethanone oxime. Anticonvulsant activity of the compounds was determined by maximal electroshock (MES) and subcutaneous metrazol (ScM) seizure tests, while neurological disorders were evaluated using rotorod toxicity test according to the ASP of NIH. Compound 1, 6 and 7 showed anticonvulsant activity at 300 mg/kg dose at 4 h, but compounds 1 and 7 showed toxicity at 300 mg/kg dose at half an hour. Antimicrobial activities of the compounds were also determined using agar microdilution method. Compound 1 and 5 were found to have the highest antifungal activity among the other compounds.

Conventional and microwave prompted synthesis, antioxidant, anticholinesterase activity screening and molecular docking studies of new quinolone-triazole hybrids

The synthesis of ethyl 4-oxo-1,4-dihydroquinoline-3-carboxylates (4, 5) was performed via the reaction of corresponding anilines with diethyl ethoxymethylenemalonate under conventional and also microwave promoted conditions. The treatment of 4 and 5 afforded the corresponding hydrazides (6 and 7). These hydrazides were converted to the corresponding carbo(thio)amides (9a-f and 10a-e) which were then subjected to an intramolecular cyclisation leading to the formation of quinolone-triazole hybrids (11a-f and 12a-e). The newly synthesized compounds were screened for their biological activities such as antioxidant capacity (AC) and acetylcholinesterase Activity. Inhibition of cholinesterases is an effective method to curb Alzheimers disease, a progressive and fatal neurological disorder. A series of some novel quinolonederivatives were designed, synthesized, and their inhibitory effects on AChE were evaluated. We obtained our compounds and determined their anticholinesterase activities according to the Ellmans method. 9b and 10c showed the best AChE inhibition with 0.48 ± 0.02 and 0.52 ± 0.07, respectively. Docking studies were performed for the most active compounds (9b, 10c) and interaction modes with enzyme active sites were determined. As a result of these studies, a strong interaction between these compounds and the active sites of AChE enzyme was revealed.

Diffusion-weighted imaging (DWI) of the liver in assessing chronic liver disease: effects of the presence and the degree of ascites on ADC values

PurposeThe aim of this study was to determine the correlation between the liver and spleen apparent diffusion coefficient (ADC) values of patients with chronic liver disease and the presence and the degree of ascites.Materials and methodIn this retrospective study, we assessed 107 patients with chronic liver disease and 39 control subjects who underwent upper abdominal MR imaging including echo-planar diffusion-weighted imaging (DWI). Among the 107 cirrhotic patients, 56 were classified as group 1, 25 as group 2, and 26 as group 3 according to the absence, the presence of minimal, and the presence of massive ascites, respectively. The scores of model for end-stage liver disease (MELD) were matched between groups as the standard reference. The liver ADC, spleen ADC, and normalized liver ADC values were compared between the control group and patients’ groups.ResultsPatients with massive ascites had significantly higher MELD score compared with the other groups. The MELD score was also significantly higher in patient groups than in control group. The liver and normalized liver ADCs of patients’ groups were significantly lower than that of the control group. With some overlap among groups, the measured ADC values decreased as the amount of the ascites increased, and these relationships were statistically significant. Furthermore, compared to control group, patients with massive ascites had significantly higher spleen ADCs.ConclusionOur results indicate that the ADC value of the liver and spleen correlates with the presence and the degree of ascites in patients with chronic liver disease, and merits further study.

The Effect of The Intercondyler Notch Width Index on Anterior Cruciate Ligament Injuries A Study on Groups with Unilateral and Bilateral ACL Injury

Objectives: To evaluate the relationship of the intercondylar notch width with unilateral and bilateral ACL injury by using MR images. Methods: The intercondylar notch width index was measured on the MR images of 18 patients with a bilateral ACL injury, 38 patients with a unilateral ACL injury and 53 healthy subjects with a normal ACL and the results of all groups were compared with each other. Results: The mean NWI values were 0.227 (±0.008) in bilateral injured; 0.245 (±0.009) in unilateral injured and 0.272 (±0.01) in control groups and 0.251(±0.01) in unaffected side of the unilateral group. There were statistically significant differences in intercondylar notch width index (NWI) values between all groups and there was a significant difference between the affected and the unaffected sides in group with unilateral ACL injury. A cutoff value of 0.25 for NWI gave an odds ratio of 26.5 for bilateral and 3.23 for unilateral ACL injuries. Conclusion: The finding that NWI is significantly narrowed in patients with bilateral and unilateral ACL tears compared with the healthy controls suggest a relationship between a narrow NWI and an increased risk of ACL injury. The patients with a narrow NWI should also be screened contralaterally for assessment of ACL injury risk on the other knee. So, specialized training programmes for the people with narrow NWI can be prepared for preventing ACL injuries.

Synthesis, anticonvulsant activity, and molecular modeling studies of novel 1-phenyl/1-(4-chlorophenyl)-2-(1H-triazol-1-yl)ethanol ester derivatives

A series of new ester derivatives were synthesized by the reaction of various acids with 1-phenyl/1-(4-chlorophenyl)-2-(1H-triazol-1-yl)ethanol and in vivo screened for their anticonvulsant activity. The title compounds were screened against MES and ScM seizure tests according to a modified version of the Epilepsy Therapy Screening Program (ETSP) protocol of the National Institutes of Health (NIH). Their neurotoxic effects were evaluated by the rotarod test. All the compounds showed protection against MES and/or ScM-induced seizures at 30 mg/kg without neurotoxicity. More compounds were found active in the ScM test and at lower dose than the MES test. Physicochemical and pharmacokinetic profiles of the compounds were predicted by QikProp. Using molecular docking approach we tried to get insights into their possible anticonvulsant mechanisms.

Cerebrospinal Fluid Dynamics in Patients with Multiple Sclerosis: The Role of Phase-Contrast MRI in the Differential Diagnosis of Active and Chronic Disease

Objective Multiple sclerosis (MS) is an inflammatory disease characterized by demyelinating plaques in the white matter. Chronic cerebrospinal venous insufficiency (CCSVI) has been proposed as a new hypothesis for the etiopathogenesis of MS disease. MS-CCSVI includes a significant decrease of cerebrospinal fluid (CSF) flow through the cerebral aqueduct secondary to an impaired venous outflow from the central nervous system. This study aimed to determine whether CSF flow dynamics are affected in MS patients and the contributions to differential diagnosis in active and chronic disease using phase-contrast magnetic resonance imaging (PC-MRI). Materials and Methods We studied 16 MS patients with chronic plaques (group 1), 16 MS patients with active plaques-enhanced on MRI (group 2), and 16 healthy controls (group 3). Quantitatively evaluation of the CSF flow was performed from the level of the cerebral aqueduct by PC-MRI. According to heart rates, 14–30 images were obtained in a cardiac cycle. Cardiac triggering was performed prospectively using finger plethysmography. Results No statistically significant difference was found between the groups regarding average velocity, net forward volume and the average flow (p > 0.05). Compared with the controls, group 1 and group 2, showed a higher peak velocity (5.5 ± 1.4, 4.9 ± 1.0, and 4.3 ± 1.3 cm/sec, respectively; p = 0.040), aqueductal area (5.0 ± 1.3, 4.1 ± 1.5, and 3.1 ± 1.2 mm2, respectively; p = 0.002), forward volume (0.039 ± 0.016, 0.031 ± 0.013, and 0.021 ± 0.010 mL, respectively; p = 0.002) and reverse volume (0.027 ± 0.016, 0.018 ± 0.009, and 0.012 ± 0.006 mL, respectively; p = 0.000). There were no statistical significance between the MS patients with chronic plaques and active plaques except for reverse volume. The MS patients with chronic plaques showed a significantly higher reverse volume (p = 0.000). Conclusion This study indicated that CSF flow is affected in MS patients, contrary to the hypothesis that CCSVI-induced CSF flow decreases in MS patients. These findings may be explained by atrophy-dependent ventricular dilatation, which may occur at every stage of MS.

Design, synthesis, and molecular modeling of new 3(2H)-pyridazinone derivatives as acetylcholinesterase/butyrylcholinesterase inhibitors

Inhibition of cholinesterases is an effective method to curb Alzheimer’s disease, a progressive and fatal neurological disorder. A series of 6-substituted-3(2H)-pyridazinone-2-acetyl-2-(p-substituted benzalhidrazone) derivatives were designed, synthesized, and their inhibitory effects on acetylcholinesterase and butyrylcholinesterase were evaluated in pursuit of potent dual inhibitors. We obtained our compounds by the reaction of various substituted/nonsubstituted benzaldehydes with 6-[4-(3,4-dichlorophenyl)piperazine-1-yl]-3(2H)-pyridazinone-2-yl acetohydrazide and determined their anticholinesterase activities according to the Ellman’s method. 5f and 5i showed 75.52 and 71.72% acetylcholinesterase inhibition at 100 µg/ml, respectively. 5h and 5f, on the other hand, were the best butyrylcholinesterase inhibitors with 67.16 and 62.03% inhibition at the same concentration, respectively. 5f emerged as a potent dual cholinesterase inhibitor. Through molecular docking studies we predicted the inhibition mechanism of 5f for both enzymes in comparison with our previous derivatives, which differ in inhibition potency, and tried to get insights into the factors that affect receptor affinity in molecular level.

Incidentally Detected Myocardial Cleft: Cardiac Computed Tomography and Magnetic Resonance Imaging Findings

Myocardial clefts are congenital anomalies, usually localized in the basal inferior wall of the left ventricle and mid-apical segments of the interventricular septum. The patients with genetic mutations related to hypertrophic cardiomyopathy showed significant elevation in the incidence of myocardial cleft. Also there is a significant correlation between the myocardial clefts and the carriers of hypertrophic cardiomyopathy gene mutations without clinical signs . Magnetic resonance imaging allows us to diagnose the myocardial clefts of the healthy individuals as well as the patients and closely follow up for clinical hypertrophic cardiomyopathy. Here we present the cardiac computed tomography and magnetic resonance imaging findings of a case with myocardial cleft.

Isolated Tuberculosis of Capitate and Triquetrum

Musculoskeletal system is involved in about 20% of the patients diagnosed with tuberculosis. Although musculoskeletal tuberculosis generally affects spine and large joints (hip and knee), hand involvement of the tuberculosis is seen in 10% of the patients with musculoskeletal involvement and also isolated tuberculosis of hand or wrist is much rarer. In the following report, we discuss the case of a 23-year-old male patient who was diagnosed with isolated tuberculosis of the capitate and triquetrum bone. The patient presented with a nonhealing sinus on the left wrist joint. Imaging revealed lytic lesions of the capitate and triquetrum. The diagnosis of tuberculosis was confirmed by histopathological examination on the bone specimen obtained from the debridement and curettage. Antituberculosis therapy was started postoperatively and 1 month later, healing of the sinus was observed. There was no sign of reactivation seen at follow-up 22 months after treatment.

Ultrasonography-Guided Injection for Quadriceps Fat Pad Edema: Preliminary Report of a Six-Month Clinical and Radiological Follow-Up

Purpose: To investigate efficacy and safety of ultrasonography-guided local corticosteroid and anesthetic injection followed by physical therapy for the management of quadriceps fat pad (QFP) edema. Materials and Methods: We prospectively evaluated 1671 knee MRI examinations in 1542 patients for QFP edema with mass effect, which was present in 109 (6.5%) knees. Participants were assigned into injection and therapy groups (both received the same physical therapy program). Injection group was first treated with ultrasonography-guided QFP injection of 1 mL corticosteroid and 1 mL local anesthetic agent. Patients were evaluated at baseline and 1-, 2-, 6-month follow-up for pain using static and dynamic visual analogue scale (VAS), suprapatellar tenderness, and QFP edema on MRI. Results: Final sample size consisted of 19 knees (injection group, 10; therapy group, 9) in 17 patients. An overall improvement was detected in both groups between baseline and final assessments. The injection group fared better than the therapy group in static VAS scores (3.33 ± 1.70 versus 0.56 ± 1.33), while there was no such difference for dynamic VAS. Incidence of suprapatellar tenderness decreased in both groups, statistically significantly in the injection group (from 100% to 0%). Pain reduction was greater in the injection group at the first month (88.9% – 90% good response versus 50% – 66.7% good response, static-dynamic VAS scoring, respectively), whereas there was no such superiority at the sixth month. No severe adverse events were identified. Conclusion: Ultrasonography-guided local injection followed by physical therapy is safe in the management of QFP edema; however, it is not superior to stand-alone physical therapy program in the long term.