Search results for "Ketone"
showing 10 items of 337 documents
A new synthetic entry into the tricyclo[3.3.0.03,7] octane skeleton
1987
Abstract A short synthesis of dimethyl tricyclo[3.3.0.03,7] octane-1,5-dicarboxylate, 13 , and its 3,7-dimethyl-derivative, 14 , by iodine oxidation of the bis-enolate derived from the corresponding dimethyl cis -bicyclo[3.3.0] octane-3,7-dicarboxylate, 11 or 12 , is described.
2-(4-Toluidino)pyrimidine
1984
Aus der Kondensation von 4-Tolylguanidin (1) mil den β-Diketonen 2a-g gehen die 2-(4-Toluidino)pyrimidine 3a-g hervor, unter denen sich Vertreter mit antidiabetischer und antimykotischer Wirksamkeit befinden. Antidiabetic Agents, II: 2-(4-Toluidino)pyrimidines Condensations of 4-tolylguanidine (1) with the β-diketones 2a-g yield the 2-(4-toluidino)pyrimidines 3a-g which comprise compounds exhibiting antidiabetic and antimycotic activities.
Antimykotische wirkstoffe. XX . Fluorierte 2-(4-toluidino)pyrimidine
1985
Aus der Kondensation von 4-Tolylguanidin (1) mit den β-Diketonen 2a-f gehen die fluorierten 2-(4-Toluidino)pyrimidine 3a-f hervor. Strukturtyp 3 zeichnet sich durch antimykotische Wirkung aus. Condensation of 4-tolylguanidine (1) with the β-diketones 2a-f yields the fluorinated 2-(4-toluidino)pyrimidines 3a-f. Structures of type 3 exhibit antimycotic activity.
Antimykotische wirkstoffe. XIX. 4,6-Disubstituierte 2-(cyanamino)pyrimidine
1985
Aus der Umsetzung von Dicyandiamid (1) mit β-Diketonen (2a-c) gehen die 2-Cyanaminopyrimidine (3a-c) hervor. Strukturtyp 3 wird durch spektroskopische Daten gestutzt, wahrend gleichzeitig eine 1-Cyan-2-imino-struktur (4) ausgeschlossen wird. Verbindung 3a zeigt fungistatische und nematizide Wirkungen. The reaction of city dicyandiamide (1) with β-diketones 2a-c leads to 2-(cyanoamino)pyrimidines 3a-c. Structure type 3 is supported by spectroscopic data, while at the same time a 1-cyano-2-imino structure (4) is excluded. Compound 3a exhibits fungistatic and nematicidal activity.
Verbindungen mit potentiell positiv inotroper Wirkung, 2. Mitt. Synthese von 3,4-Dihydro-2-[(3-oxo-1-cyclopenten-1-yl)amino]-1(2H)-phenanthron und 3-…
1984
Die Darstellung der Titelverbindungen aus 1,3-Cyclopentandion und 2-Amino-3,4-dihydro-1(2H)-phenanthron bzw. 2-Amino-1,2,3,4-tetrahydro-1-phenanthrol wird beschrieben. Compounds with Potentially Positive Inotropic Activity, II: Synthesis of 3,4-Dihydro-2-[(3-oxo-1-cyclopenten-1-yl)amino]-1(2H)-phenanthrone and 3-(1,2,3,4-Tetrahydro-1-hydroxy-2-phenanthrylamino)-2-cyclopentenone The synthesis of the title compounds from 1,3-cyclopentanedione and 2-amino-3,4-dihydro-1(2H)-phenanthrone and 2-amino-1,2,3,4-tetrahydro-1-phenanthrole is described.
Hypolipidaemic effects of fenofibrate are not altered by mildronate-mediated normalization of carnitine concentration in rat liver.
1999
The five-fold higher carnitine content in the liver of fenofibrate-treated rats addresses the question about the possible role of this enhancement in the hypolipidaemic effect of the drug and the underlying mechanisms. When fenofibrate was administered with mildronate (a gamma-butyrobetaine hydroxylase inhibitor) in suitable amount, the content in carnitine was found to be normalized in liver. However, triglyceride contents of liver and serum were then at least as low as in rats treated by fenofibrate only. When carnitine concentration was lowered by mildronate to the third of the normal value, a marked increase in triglycerides occurred both in liver and serum, while the five-fold increase…
Mildronate: An Antiischemic Drug for Neurological Indications
2005
Mildronate (3-(2,2,2-trimethylhydrazinium)propionate; MET-88; meldonium, quaterine) is an antiischemic drug developed at the Latvian Institute of Organic Synthesis. Mildronate was designed to inhibit carnitine biosynthesis in order to prevent accumulation of cytotoxic intermediate products of fatty acid beta-oxidation in ischemic tissues and to block this highly oxygen-consuming process. Mildronate is efficient in the treatment of heart ischemia and its consequences. Extensive evaluation of pharmacological activities of mildronate revealed its beneficial effect on cerebral circulation disorders and central nervous system (CNS) functions. The drug is used in neurological clinics for the trea…
Physico-chemical stability of eribulin mesylate containing concentrate and ready-to-administer solutions.
2013
Objectives The aim of this study was to determine the stability of commercially available eribulin mesylate containing injection solution as well as diluted ready-to-administer solutions stored under refrigeration or at room temperature. Methods Stability was studied by a novel developed stability-indicating reversed-phase high-performance liquid chromatography (RP-HPLC) assay with ultraviolet detection (detection wavelength 200 nm). Triplicate test solutions of eribulin mesylate containing injection concentrate (0.5 mg/mL) and with 0.9% sodium chloride solution diluted ready-to-administer preparations (0.205 mg/mL eribulin mesylate in polypropylene (PP) syringes, 0.020 mg/mL eribulin mesyl…
Eribulin Mesylate for the Treatment of Metastatic Hormone-refractory and Triple-negative Breast Cancer: A Multi-institutional Real-world Report on Ef…
2021
Objective Eribulin mesylate (EM) is a fully synthetic macrocyclic ketone analogue of the marine natural product halichondrin. EM has been reported to be active in metastatic breast cancer. In this paper, we report efficacy and safety of data of EM in a retrospective, real-world series of patients with poor prognosis, hormone-refractory, or triple-negative metastatic breast cancer. Materials and methods The analysis was carried out at 4 interrelated oncology centers. EM was delivered at the dose of 1.4 mg/m2 in 100 mL of normal saline over 2 to 5 minutes on days 1 and 8 every 21 days. EM was continued until disease progression or unacceptable toxicity. Side effects were reported every cycle …
Staurosporine-induced apoptosis in Chang liver cells is associated with down-regulation of Bcl-2 and Bcl-XL.
2004
A potent inhibitor of serine/threonine kinases, staurosporine exerts antiproliferative and apoptotic effects in many cancer cells, although the exact mechanism of its action is still unclear. This study examines the effects of staurosporine on Chang liver cells, an immortalized non-tumor cell line, in comparison with those caused in HuH-6 and HepG2 cells, two human hepatoma cell lines. Our results provide evidence that staurosporine promotes apoptosis in Chang liver cells as observed by flow cytometric analysis and acridine orange/ethidium bromide staining. The effect appeared already after 8 h of treatment and increased with treatment time and dose. After 48 h of exposure to 200 nM stauros…