Synthesis,Decarboxylation, and Nitrosation of 1-Acyl-2-pyrrolidone-3-carboxylic Acids: A Convenient Novel Entry to 2,3-Dioxopyrrolidine Derivatives

Esters 1 of 1-acyl-2-pyrrolidone-3-carboxylic acids 2 were hydrolized to 2 with acetic acid/HCl at 60–70°C. Reaction of 1a with formic acid/HCl at 60–75°C led to (not isolated) 2a which began to decarboxylate to 3a during the conversion of 1a to 2a even at this low temp. Decarboxylation of 2c-f was accomplished at 160°C without solvent. Decarboxylative nitrosation of 2c-f yielded the oximes 4c-f of 1-acyl-2,3-dioxopyrrolidines. Treatment of 4f with magic methyl provided the enol ether 5f of the respective dioxopyrrolidine.     

4. Synthesis,metabolism and release of histamine

Inflammation Research - .     

α galnac is essential for recognition of EXO-1 epithelial antigen by mouse monoclonal antibody Pa-G-14

Mouse monoclonal antibody Pa-G-14 detects Exo-1, an antigen whose expression is regulated in the processes of epithelial-cell differentiation and transformation. The epitope recognized by Pa-G-14 is present both in glycosphingolipids and in mucin glycoproteins. To characterize the specificity of Pa-G-14, immuno-thin-layer chromatography, biochemical, and enzymatic treatment of glycosphingolipid extracts from human pancreas were used. The antibody bound to all blood-group-A substances; αGaINAc, but not fucose, was essential for reactivity. In ELISA, Pa-G-14 also reacted with ovine and bovine submaxillary mucins but not with porcine submaxillary mucin. Binding to ovine submaxillary mucin was resistant to neuraminidase treatment. In solid-phase absorption assays on synthetic carbohydrate structures, Pa-G-14 recognized broadly blood group A, Tn and sialyl-Tn. Using immuno-electron-microscopic techniques, reactivity with all Golgi cisternae and mucin droplets of mucous cells in ovine submaxillary gland was demonstrated. All these assays indicate that Pa-G-14 shows a novel specificity, since it binds blood group A, Tn and sialyl-Tn, the common structural feature of these epitopes being the presence of a terminal αGalNAc sugar unit.     

Fibromuseular dysplasia of the internal carotid artery in a child with alpha-1-antitrypsin deficiency

Fibromuseular dysplasia (FMD) is a non-inflammatory segmental arteriopathy of unknown origin. Most often the renal arteries are affected, however, also mesenteric, lumbar, vertebral, or carotid arteries may be Involved. FMD has frequently been reported as a cause of stroke in adults, but very rarely in children. We report the case of an 11-year-old boy who presented with an ischaemic infarction in the anterior part of the territory of the left middle cerebral artery. Angiography demonstrated a'string of beads'lesion suggestive of FMD causing occlusion at the origin of the middle artery. Laboratory analyses revealed the protease inhibitor (Pi) phenotype SZ (PiSZ) of alpha-1-antitrypsin deficiency as well as decreased antioxidants and signs of enhanced lipid peroxidation. Such an imbalance may be associated with diminished resistance to oxidation, possibly causing direct cellular and tissue injury. Whether alpha-1-antitrypsin deficiency and an impaired status of antioxidants, as seen in our patient, might play a role in the pathogenesis of FMD is presently unclear.     

Resorbierbare Calciumphosphatkeramik im Tierexperiment unter Belastung

Zusammenfassung Segmentscheiben aus keramischen Werkstoffen auf der Basis von Tricalcium- bzw. Tetracalciumphosphat mit einem durchgehend offenen System von Röhrenporen von 45 Vol- % wurden anstelle einer herausgesÄgten 7 mm dicken Knochenscheibe in die Tibia von Hunden implantiert. Nach Abnahme der Fixierung nach 12 Wochen belasteten die Hunde in physiologischer Weise die operierten Gliedmaßen. Histologisch wurde festgestellt, daß die Osteotomiespalten mit der Keramik primär verheilt waren. Die Tricalciumphosphatkeramik war nach 10 Monaten weitgehend resorbiert und durch Knochengewebe ersetzt. Die Tetracalciumphosphatkeramik war dagegen vollständig erhalten und in den Poren von lamellärem Knochengewebe durchwachsen, das sich dicht und bindegewebsfrei auf der Keramik auflagerte. Zwischen Knochen und Keramik bestand ein mechanisch nicht lösbarer Verbund.Die untersuchten Keramiken waren gewebeverträglich und sind u. E. geeignet, die heute verwendeten Knochentransplantate z.T. zu ersetzen. Tricalciumphosphatkeramik ist an Stellen einsetzbar, an denen keine extremen Belastungen auftreten; Tetracalciumphosphatkeramik ist mechanisch stabiler und könnte auch für höher belastete permanente Implantate verwendet werden.

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Resorbable calcium phosphate ceramics under load

Summary Cylindrical implants with 45 % by volume continuous open tubular pores were prepared from ceramic materials based on tricalcium and tetracalcium phosphate and used to replace 7 mm thick bone segments in the tibiae of dogs. The treated limbs of the experimental animals were fixed for 12 weeks, after which time the dogs were allowed to move freely so that the limbs were physiologically loaded. The histological examination showed that primary bone healing had taken place between the bone and the ceramic material. After 10 months the tricalcium-phosphate-based ceramic material was resorbed and replaced by bone tissue to a large extent. The ceramic material on the basis of tetracalcium phosphate, on the other hand, had remained completely unchanged, and its pores were filled with lamellar bone tissue which was in direct contact with the implant without connective tissue. The bond between natural bone and implant was mechanically stable.The ceramic materials investigated were found to be tissue-compatible, and in our opinion they can be substituted for part of the bone transplants used today. Considering its varying strength properties, the tricalcium phosphate ceramic material can be used only in cases where no high stress is expected; the tetracalciumphosphate-based ceramic material, however, has a higher mechanical strength and can therefore be used also for larger permanent implants which have to bear high mechanical stress.

Die Untersuchungen sind Teil einer Forschungsarbeit, die das Battelle-Institut, Frankfurt am Main, im Aufrage des Bundesministeriums für Forschung und Technologie durchführte     

Urge incontinence in the elderly – supraspinal reflex incontinence

World Journal of Urology -     

Familial Aggregation of Spelling Disability

This study examined the familial aggregation of spelling disability in a sample of 32 German school-aged children and their relatives. The influence of two different diagnostic criteria (low-achievement criterion, and regression-based IQ-discrepancy criterion) on the rate of affectedness was investigated. Results revealed that 52.3-61.9% of the sibs and 26-34% of the parents were spelling disabled. Little evidence was found for an influence of the diagnostic criterion on the rate of affectedness.     

Clonidine Suppression Test Revisited

Background: The diagnosis of pheochromocytoma may be difficult because the clinical picture is variable. Objective: The purpose of this paper is to report our experience and to review the published data on the diagnostic significance and risks of the clonidine suppression test in the diagnosis of pheochromocytoma. Patients and Methods: 114 patients were evaluated for pheochromocytoma using the clonidine suppression test. Results: The diagnosis was established in four patients. Overall accuracy of the test in our own series was 98% when the normal response to clonidine was defined as total plasma catecholamines of less than 500 ng/L, or less than 70% of the baseline value. No serious complication was noted. Conclusion: Our data and the published series demonstrate that the clonidine suppression test is accurate and safe in patients with suspected pheochromocytoma.     

Protoberberine aus Reissert-Verbindungen, 2. Mitt.: Eine neue Synthese von 8-Methyldibenzo[a,g]chinolizidinen

Protoberberines from Reissert Compounds, II: A New Synthesis of 8-Methyldibenzo[a,g]quinolizidines The Reissert compounds 16 are benzylated by 2-bromomethylacetophenone dioxolane 14 to give the dihydroisoquinolines 5 . Treatment of 5 with KOH yields the 1-benzylisoquinolines 6 which spontaneously form the deoxygenated coralynes 4 in acidic solution. 4a and 18 are reduced by NaBH₄ to give the 8-methyl-trans-dibenzoquinolizidines 19 . The sequence 5 → 6 → 4 → 19 is a new efficient access to coralyne analogues and 8-substituted tetrahydroprotoberberines.- Bromination of 2-methylacetophenone does not lead to 2-bromomethylacetophenone but to the benzalbromide 9 or to the phenacylbromide 11 .