Synthesis and kinetics studies of N′‐(2‐(3,5‐disubstituted‐4H‐1,2,4‐triazol‐4‐yl)acetyl)‐6/7/8‐substituted‐2‐oxo‐2H‐chromen‐3‐carbohydrazide derivatives as potent antidiabetic agents

A novel series of N′‐(2‐(3,5‐disubstituted‐4H‐1,2,4‐triazol‐4‐yl)acetyl)‐6/7/8‐substituted‐2‐oxo‐2H‐chromen‐3‐carbohydrazides were synthesized and studied for their α‐glucosidase inhibition activity. Most of the synthesized compounds exhibited potential α‐glucosidase inhibition activity with IC₅₀ values ranging from 0.96 ± 0.02 to 32.86 ± 0.73 µg/ml. Among them, compounds 3e and 4e , having a methoxy group on the coumarin ring, proved to be the most potent ones, showing an enzyme inhibition activity with IC₅₀ = 0.96 ± 0.02 and 1.44 ± 0.06 µg/ml, respectively. The kinetic study through Lineweaver–Burk plots revealed that the inhibition mechanism of the most active compounds 3d, 3e, 4d , and 4e , on the α‐glucosidase activity, was found to be in the competitive mode.     

Multifocal intradiploic cavernous hemangioma of the skull associated with nasal osteoma

Summary.  Objective: To present a 42-year-old female patient with multifocal cavernous hemangioma of the skull associated with nasal osteoma.  Design: A case report.  Intervention methods: X-rays, computerized tomography, magnetic resonance imaging, and histopathology were used to achieve the diagnosis of this rare entity. The multiple cavernous hemangiomas were resected en-bloc and a curettage biopsy was obtained from the nasal osteoma.  Results: The patient healed well after the operation. No recurrences of the cavernous hemangiomas were observed after one-year follow-up.  Conclusion: Multifocal cavernous hemangiomas are rare benign lesions of the calvarium, arising from the intrinsic vasculature of the bone. Although they are benign, radiological findings are not always characteristic and their multiple presentation may easily make surgeons consider the other malignancies of the skull in the differential diagnosis. Histopathologic confirmation of the tumor is the definitive method for diagnosis. The treatment of choice is early en bloc resection of the tumour where it is possible. Published online April 28, 2003  Correspondence: Kayhan Kuzeylı˙, M.D., Karadeniz Teknik U¨niversitesi, Farabi Hastanesi N?roşirurji AbD, 61080 Trabzon, Türkiye.     

Ruptured chronic encapsulated intracerebral hematoma in infancy: review of the literature with a case report

Objectives We report a case of a 2-month-old boy with chronic encapsulated intracerebral hematoma (EICH) and discuss clinical, radiological and pathological features of the case.Conclusions Chronic EICH in infants is extremely rare in the literature. Only two cases have been previously reported. One of the cases reported in the literature was supratentorial and the other was infratentorial.     

Spontaneous thrombosis of vein of Galen aneurysmal malformation after ventriculoperitoneal shunting.

Aneurysmal dilatation of the vein of Galen (AVG) is a common finding in vascular malformations that involve the Galenic system and spontaneous thrombosis is very rare. Although the presentation of the cases may differ with the age, the mortality and morbidity is high in all age groups. Here, we present a case of AVG in a six-month-old boy. The patient underwent insertion of a ventriculoperitoneal shunt. Surveillance of the lesion with subsequent MRI revealed spontaneous thrombosis of the AVG with excellent clinical outcome. Proposed mechanisms of spontaneous thrombosis include slow flow shunts, obstruction of the venous outflow or obstruction of the feeding artery. The case is discussed with the relevant literature.     

Effects of clotrimazole on experimental spinal cord injury

BACKGROUND: We examined a possible neuroprotective effect of clotrimazole on spinal cord clip compression injury. METHODS: Rivlin and Tator's acute extradural clip compression injury (CCI) model was used for producing SCI on 24 albino Wistar rats weighing 180-250 g. All rats were anesthetized with 30 mg/kg ketamine HCl intraperitoneally and were breathing spontaneously without tracheal intubation. Total laminectomy of T8-T12 was performed on all rats under operation microscope, and CCI was performed on all rats (expect those in group 1) with a 50-g closing force aneurysm clip for 1 min. Three hours later, all of the rats were killed with sodium pentobarbital. Spinal cords were excised for a length of 2 cm; 1 cm rostrally and caudally to the injury site and deep frozen at -76 degrees C for biochemical studies. RESULTS: Treatment with clotrimazole decreased MDA levels in rats with SCI with a statistically significant difference. CONCLUSIONS: To our knowledge, this the first study that shows the effects of clotrimazole on spinal cord clip compression injury. Clotrimazole was found to be effective on spinal cord clip compression injury, but further investigations are mandatory.     

The effects of tyrphostine Ag 556 on experimental spinal cord ischemia reperfusion injury

BACKGROUND: To investigate the effects of Tyrphostin Ag 556 on spinal cord ischemia reperfusion injury. METHODS: The inhibition of tyrosine kinase may represent a novel approach in the treatment of spinal cord ischemia reperfusion injury. Recently, a family of tyrosine kinase inhibitors, the tyrphostins, has been successfully used in models of endotoxemia, peritonitis, and hypovolemic shock. MATERIALS AND METHODS: Twenty-four Wistar rats were used in the study. Rats were divided into 4 groups of 6 animals. The groups were named as sham operated group, injury group, vehicle group, and treatment group. Clamping of the abdominal aorta was performed for 45 minutes with all of the groups except sham-operated group. All of the rats were sacrificed 24 hours after the operation for biochemical and ultrastructural studies. RESULTS: Tyrphostin Ag 556 treatment was found effective on experimental spinal cord ischemia reperfusion injury. The Malondialdehyde (MDA) values of the treatment group were statistically significant lower then the other reperfusion injury groups. The histologic examination showed better cellular structure in the treatment group than the other reperfusion injury groups. The neurologic scores of the treatment group also improved after treatment. CONCLUSIONS:Tyrphostin Ag 556 alters spinal cord ischemia reperfusion injury by inhibiting protein kinases. Further investigations will be required to determine the long-term effects of this drug.     

Effects of citicoline on experimental spinal cord injury.

OBJECTIVE: To investigate the effects of citicoline on experimental spinal cord injury (SCI). BACKGROUND: Citicoline has been successfully used in clinical studies of head injury and cerebral infarction, but there is limited literature regarding its use in experimental SCI. STUDY DESIGN: Twenty adult Wistar rats were divided into four groups: sham, trauma, vehicle, and citicoline-treated. SCI was produced using a weight drop technique. Citicoline 300 mg/kg was given intraperitoneally, 5 minutes after the induction of trauma. The animals were sacrificed and 1 cm long samples of injured spinal cord were obtained at 48 hours post-SCI. Lipid peroxidation was estimated by the thiobarbituric acid test. Neurological examinations were performed using a previously described grading scale. RESULTS: Measures of lipid peroxidation and motor scores of the citicoline-treated group were significantly lower than those in the other injury groups. CONCLUSIONS: Citicoline attenuated lipid peroxidation after SCI and improved the motor scores. Further investigations will be required to determine the long-term effects of this drug on spinal cord injury.     

Shunt dysfunction due to calcification of a ventriculo-peritoneal shunt: a case report.

Calcification and related dysfunction of ventriculo-peritoneal shunts are rare events in neurosurgical practice. Shunt calcification causes shunt dysfunction in two ways, namely disconnection and obstruction.We present a 16-year-old girl with shunt malfunction due to disconnection secondary to calcification. The shunt tubing fractured during attempted removal and some of the remaining components, including the ventricular catheter, had to be left in situ. The shunt was revised and the patients symptoms resolved. Replacement of the calcified and perished shunt components with a new shunt is essential. Aggressive surgical manipulation for removal of the remaining shunt components is not advisable as this may increase morbidity and mortality.     

Convenient synthesis of fused heterocyclic 1,3,5-triazines from some N-acyl imidates and heterocyclic amines as anticancer and antioxidant agents

N-Acyl imidates (2), reacting with 5-amino pyrazole (3), 2-aminobenzimidazole (4), 3-amino-1,2,4-triazole (5), 3,5-diamino-1,2,4-triazole (6), and 5-aminotetrazole (7) give pyrazolo[1,5-a][1,3,5]triazine (8), benzo[4,5]imidazo[1,2-a][1,3,5]triazine (9), [1,2,4]triazolo [2,3-a][1,3,5]triazine (10), [1,2,4]tri azolo[2,3-a][1,3,5]triazin-5-ylamine (12), and tetrazolo-[1,5-a][1,3,5]triazine (14) derivatives, respectively. The synthesized compounds were characterized on the basis of IR, (1)H-NMR, (13)C-NMR, and mass spectral data and elemental analyses results. Five of the newly synthesized compounds, 8a, 9a, 10a, 12a, and 14a, were selected by National Cancer Institute and screened for their anticancer activity against three cancer cell lines MCF7, NCI-H460, and SF-268, where 12a exhibited moderate anti-proliferation potential. 12a was, thus, further tested for anticancer activity against 60 human cancer cell lines and showed moderate growth inhibition potency. 12a showed a high growth inhibitory activity against A498 renal cancer cell line. All of the newly synthesized compounds 8-10, 12 and 14 were tested for their antioxidant capacity where they exhibited very high activity, even higher than the widely used reference antioxidants butylated hydroxytoluene and 6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid (Trolox). Compound 12a also showed the highest antioxidant activity.