Search results for "Azoles"
showing 10 items of 899 documents
Dopamine agonists in schizophrenia: a review.
1995
Although it is unlikely that the different types of course and severity of schizophrenia are caused by one neurochemical abnormality alone, indirect pharmacological evidence still suggests a relative excess of dopaminergic activity being implicated in the pathogenesis of most of the schizophrenic symptoms, e.g. positive symptomatology. Synthesis and release of dopamine as well as firing rates of dopaminergic neurons are controlled by stimulation of autoreceptors via a negative feedback regulation. Investigations on therapeutic effects of autoreceptor-nonselective dopamine agonists in schizophrenia have yielded inconsistent results. Dopamine autoreceptor agonists like pramipexole, roxindole,…
Brimonidine versus dapiprazole: Influence on pupil size at various illumination levels.
2005
To evaluate the influence of dapiprazole versus brimonidine on pupil size at various illumination levels.Department of Ophthalmology, Johannes Gutenberg-University, Mainz, Germany.In randomized prospective study, 19 healthy volunteers received 2 ophthalmic solutions, dapiprazole and brimonidine, 1 in each eye, for intraindividual comparison. Before and after application, pupil diameter was measured using an infrared binocular pupillometer at 3 illumination levels (0.03, 0.82, and 6.4 lux).Only slight pupil dilation was observed under scotopic conditions after application of both agents. After 20 minutes, the median reduction in pupil width was 1.4 mm for brimonidine and 0.9 mm for dapiprazo…
Novel Combination of Sorafenib and Celecoxib Provides Synergistic Anti-Proliferative and Pro-Apoptotic Effects in Human Liver Cancer Cells
2013
Molecular targeted therapy has shown promise as a treatment for advanced hepatocellular carcinoma (HCC). Sorafenib, a multikinase inhibitor, recently received FDA approval for the treatment of advanced HCC. However, although sorafenib is well tolerated, concern for its safety has been expressed. Celecoxib (Celebrex®) is a selective cyclooxygenase-2 (COX-2) inhibitor which exhibits antitumor effects in human HCC cells. The present study examined the interaction between celecoxib and sorafenib in two human liver tumor cell lines HepG2 and Huh7. Our data showed that each inhibitor alone reduced cell growth and the combination of celecoxib with sorafenib synergistically inhibited cell growth an…
Dexrazoxane shows cytoprotective effects in zoledronic acid-treated human cells in vitro and in the rabbit tibia model in vivo
2012
Abstract Introduction Bisphosphonates are important and effective drugs in oncology and osteoporosis therapy. They accumulate in the bone matrix becoming released and active by bone resorption. This leads to effective inhibition of tumor cells and bone degradation. A side effect of bisphosphonates similar to other drugs like denosumab is osteonecrosis of the jaws (ONJ). This problem mostly occurs after tooth extraction. We studied the cytoprotectant dexrazoxane known from anthracycline chemotherapy for cytoprotection in nitrogen-containing bisphosphonate treated cells and in the rabbit tibia model to evaluate a possible value in ONJ management. Materials & methods Human osteoblasts (HOB) P2…
Salts of 5-amino-2-sulfonamide-1,3,4-thiadiazole, a structural and analog of acetazolamide, show interesting carbonic anhydrase inhibitory properties…
2015
Three salts of 5-amino-2-sulfonamide-1,3,4-thiadiazole (Hats) were prepared and characterized by physico-chemical methods. The p-toluensulfonate, the methylsulfonate, and the chlorhydrate monohydrate salts of Hats were evaluated as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors (CAIs) and as anticonvulsants and diuretics, since many CAIs are clinically used as pharmacological agents. The three Hats salts exhibited diuretic and anticonvulsant activities with little neurotoxicity. The human (h) isoforms hCA I, II, IV, VII, IX, and XII were inhibited in their micromolar range by these salts, whereas pathogenic beta and gamma CAs showed similar, weak inhibitory profiles.
COX-2 expression in chondrosarcoma: A role for celecoxib treatment?
2010
Chondrosarcomas are resistant to conventional chemo- and radiotherapy. A subset of chondrosarcomas arises secondarily in the benign tumour syndromes enchondromatosis (EC) and multiple osteochondromas (MO), and prevention of tumour development would greatly improve prognosis. We therefore investigated the effect of selective COX-2 inhibition on chondrosarcoma growth. COX-2 expression was studied in central- and peripheral cartilaginous tumours. The effect of COX-2 inhibition was assessed in four high-grade chondrosarcoma cell lines using celecoxib and NS-398 treatment. COX-2 activity (prostaglandin E-2 (PGE(2)) ELISA) and cell viability were measured. The (prophylactic) effect of celecoxib o…
COMPliance and Arthralgia in Clinical Therapy: the COMPACT trial, assessing the incidence of arthralgia, and compliance within the first year of adju…
2014
5 Office-based Professional Association Gynecologic Oncologists e.V. in Germany (BNGO e.V.), Berlin; 6 Background: This prospective study evaluated the relationship between arthralgia and compliance during the first year of adjuvant anastrozole therapy in postmenopausal women with hormone receptor-positive early breast cancer. Patients and methods: COMPliance and Arthralgia in Clinical Therapy (COMPACT) was an open-label, multicenter, noninterventional study conducted in Germany. Patients had started adjuvant anastrozole 3-6 months before the study start. The primary end points were arthralgia, compliance, and the relationship between compliance and arthralgia, assessed at specific time poi…
Síntesis y caracterización de compuestos de Cu(II) con derivados triazólicos. Estudio de su actividad como potenciales nucleasas químicas
2014
The main goal of this PhD thesis concerns the development of artificial metallonucleases based on copper(II)-1,2,4-triazole compounds. In order to do so, we have obtained metal compounds of different nuclearities by reaction of a new family of 1,2,4-triazole ligands with copper(II) salts. The ligands own the characteristic triazole properties upon coordinating to metals and also integrate DNA binding units (aromatic moieties) with the aim of increasing the affinity of the corresponding metal complexes to double strand DNA. We have also chosen the copper(II) ion due to its intrinsic redox and coordination properties. Here we present our conclusions in relation with their structure/activity a…
OXADIAZOLE DERIVATIVES FOR THE TREATMENT OF GENETIC DISEASES DUE TO NONSENSE MUTATIONS
2018
Are disclosed oxadiazole derivatives, their use as medicaments and in particular for the treatment of diseases associated with the presence of a nonsense mutation in the gene or a premature stop codon in the mRNA, pharmaceutical formulation comprising said oxadiazole derivatives and prodrug or mixture thereof and the methods for the preparation of said Oxadiazole derivatives.
Recent Advances in the Chemistry of 1,2,4-Oxadiazoles
2015
1,2,4-Oxadiazoles experienced an almost 80-year long period of scientific lethargy before they tickled the curiosity of chemists. The study of chemical and photochemical reactivity of 1,2,4-oxadiazoles opened the way to a series of applications in heterocyclic synthesis. Today, 1,2,4-oxadiazoles are known in medicinal chemistry for their use as bioisosters of esters and amides. Furthermore, fluorinated 1,2,4-oxadiazoles have been applied in materials science either by themselves or for the targeted modification of polymers and macromolecules. Overall, the synthesis of 1,2,4-oxadiazoles can be planned to fine-tune their properties for featured applications. Their versatility, either as start…