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New Substances (new + substance)
Selected AbstractsPladienolides, New Substances from Culture of Streptomyces platensis Mer-11107.CHEMINFORM, Issue 31 2004Part 2. No abstract is available for this article. [source] Current concepts for the prevention of venous thromboembolismEUROPEAN JOURNAL OF CLINICAL INVESTIGATION, Issue 2005P. Bramlage Abstract Venous thromboembolism (VTE) is a major cause of morbidity and mortality worldwide and the annual incidence of VTE is 1 per 1000. The individual risk for venous thromboembolism may be substantially higher and is determined by expositional and dispositional factors. Unfractionated heparin and warfarin have been the mainstays for the prevention of VTE until the early 1980s. Bleeding complications and side effects limited the use of these agents and subsequently low molecular weight heparins (LMWH) were introduced into clinical practice. These are most commonly used for the prophylaxis and treatment of VTE today. In the last decade, the pace of development of further anticoagulants has accelerated with the introduction of new treatment regimens and new substances. In this context, novel drugs directed against clotting factor Xa (such as fondaparinux) and direct thrombin inhibitors (such as melagatran/ximelagatran) have been developed. Fondaparinux shows a favourable efficacy/safety profile and has been documented to be cost-effective compared to enoxaparin in the US and the UK. [source] Methylone and mCPP, two new drugs of abuse?ADDICTION BIOLOGY, Issue 4 2005M. Bossong Recently, two new ecstasy-like substances, methylone and mCPP, were found in street drugs in the Netherlands by the Drugs Information and Monitoring System (DIMS). Methylone (3,4-methylenedioxymethcathinone) is the main ingredient of a new liquid designer drug that appeared on the Dutch drug market, called ,Explosion'. mCPP (meta-chlorophenylpiperazine) is a substance often used as a probe for the serotonin function in psychiatric research, and has now been found in street drugs, both in tablets and powders. Methylone as well as mCPP act on monoaminergic systems, resembling MDMA (3,4-methylenedioxymethamphetamine), with mCPP mainly affecting the serotonin system. The subjective effects of both new substances exhibit subtle differences with those of MDMA. Only little is known about the harmfulness of both methylone and mCPP. However, because of similarities between these substances and MDMA, risks common to MDMA cannot be excluded. [source] A11. UV-related skin hazards: allergic photodermatitisJOURNAL OF COSMETIC DERMATOLOGY, Issue 2 2002Paolo Pigatto Cases of dermatitis induced by exposure to ultra-violet radiation are increasingly encountered in clinical practice, with contact allergic photodermatitis accounting for about 10% of cases. Its frequency seems to be increasing, not only as a result of the increased use of cosmetic products and contact with some of the materials of working processes, but above all because of the greater exposure to both natural and artificial sources of UV radiation. Many substances have been defined ,photo-allergising' but their exact prevalence has varied over the years with the introduction and use of new substances in cosmetics and pharmaceutical products. For these, and other reasons, there are few studies concerning the prevalence and incidence of contact allergic photodermatitis in Italy. A total of 2160 patients with clinical histories suggestive of photoallergic contact dermatitis were seen. All patients underwent photopatch tests with haptens proposed by the Gruppo Italiano Ricerca Dermatiti da Contatto plus other substances suggested by each patient's history. 518 patients (24%) were positive to at least one test substance of the standard series or to added substances. Typical photoallergic reactions were seen in 423 subjects, representing 19.5% of the total population. Topical drugs are the substances most frequently involved in photodermatitis. The incidence in our population was about equal for antimicrobial agents, additives to fragrances, and fragrances themselves. Other allergens frequently found were sun screening agents which were the second group of haptens with clear-cut relevance. [source] What determines the molecular composition of abnormal protein aggregates in neurodegenerative disease?NEUROPATHOLOGY, Issue 4 2008Richard A. Armstrong Abnormal protein aggregates, in the form of either extracellular plaques or intracellular inclusions, are an important pathological feature of the majority of neurodegenerative disorders. The major molecular constituents of these lesions, viz., ,-amyloid (A,), tau, and ,-synuclein, have played a defining role in the diagnosis and classification of disease and in studies of pathogenesis. The molecular composition of a protein aggregate, however, is often complex and could be the direct or indirect consequence of a pathogenic gene mutation, be the result of cell degeneration, or reflect the acquisition of new substances by diffusion and molecular binding to existing proteins. This review examines the molecular composition of the major protein aggregates found in the neurodegenerative diseases including the A, and prion protein (PrP) plaques found in Alzheimer's disease (AD) and prion disease, respectively, and the cellular inclusions found in the tauopathies and synucleinopathies. The data suggest that the molecular constituents of a protein aggregate do not directly cause cell death but are largely the consequence of cell degeneration or are acquired during the disease process. These findings are discussed in relation to diagnosis and to studies of to disease pathogenesis. [source] Synthesis and insecticidal activity of new 3-benzylfuran-2-yl N,N,N,,N,-tetraethyldiamidophosphate derivativesPEST MANAGEMENT SCIENCE (FORMERLY: PESTICIDE SCIENCE), Issue 8 2008Vanderlúcia F Paula Abstract BACKGROUND: A series of 3-benzylfuran-2-yl N,N,N,,N,-tetraethyldiamidophosphate derivatives were synthesized as potential new agents to control insects. Their structures were confirmed on the basis of IR, NMR and MS analyses. RESULTS: Ten 3-benzylfuran-2-ylN,N,N,,N,-tetraethyl derivatives were prepared from the compound furan-2-yl N, (N,N,N,,N,-tetraethyldiamidophosphate). The contact toxicity of all derivatives, at a dose of 10 µg mg,1 insect, was evaluated against four insect species, Ascia monuste orseis Latr. (Lepidoptera: Pyralidae), Diaphania hyalinata (L.) (Lepidoptera: Pyralidae), Sitophilus zeamais Mots. (Coleoptera: Bruchidae) and Solenopsis saevissima (Smith) (Hymenoptera: Formicidae). The mortality range observed for some derivatives, such as 3-(3-methylbenzyl)furan-2-yl N,N,N,,N,-tetraethyldiamidophosphate (82.5% mortality against D. hyalinata; 100% mortality against S. saevissima), was comparable with that of the commercial insecticide chlorpyrifos-methyl. The biological activity of the derivatives depended on the substitution pattern of the benzylic ring. Furan-2-yl N,N,N,,N,-tetraethyldiamidophosphate, furan-2-yl N,N -diethylamidochlorophosphate and difuran-2-yl N,N -diethylamidophosphate were also evaluated, displaying, in some cases, activity comparable with that of chlorpyrifos-methyl (90%, 100% and 97.5% respectively against A. monuste orseis). Considerable activity was observed for some furan-2(5H)-ones evaluated. CONCLUSION: Ten 3-benzylfuran-2-yl N,N,N,,N,-tetraethyldiamidophosphate derivatives were synthesized and fully characterized from a chemical point of view. The results obtained from the biological assays indicate that this class of compounds can be utilized for the design of new substances endowed with insecticidal activity. Copyright © 2008 Society of Chemical Industry [source] Synthesis and antibacterial properties of peptidyl derivatives and cyclopeptides structurally based upon the inhibitory centre of human cystatin C: Dissociation of antiproteolytic and antibacterial effectsAPMIS, Issue 7-8 2000FRANCISZEK Kasprzykowski Cysteine protease-inhibiting proteins of the cystatin superfamily can inhibit the replication of certain viruses and bacteria. The inhibitory centre of human cystatin C, the most widely distributed human cystatin, comprises three peptide segments. The present work describes the synthesis and antibacterial activity of 27 new peptidyl derivatives or cyclopeptides based upon the aminoterminal segment Arg8 -Leu9 -Val10 -Gly11. Fourteen of the new compounds displayed antibacterial activity against from 1 up to 9 of 17 clinically important bacterial species tested. Antiproteolytic activity of a compound was usually not required for its antibacterial capacity. Peptidyl diazomethanes generally had a very narrow antibacterial spectrum, inhibiting only Streptococcus pyogenes, whereas cyclopeptides and peptidyl derivatives of the general structure X-Arg-Leu-NH-CH(iPr)-CH2 -NH-Y had a much wider spectrum. The most potent of these substances displayed approximately equal minimal inhibitory and bactericidal concentrations of about 20 ,g/ml for both Staphylococcus aureus and S. pyogenes and were devoid of antiproteolytic activity. Several of the new substances could protect mice against lethal intraperitoneal challenge with S. pyogenes. Though their target remains to be disclosed, the group of substances here reported might be promising for the development of antibacterial drugs and the discovery of novel principles of action. [source] Gase als zelluläre Signalstoffe.BIOLOGIE IN UNSERER ZEIT (BIUZ), Issue 3 2010Gasotransmitter Abstract Die Gase Stickoxid (NO), Kohlenmonoxid (CO) und Schwefelwasserstoff (H2S) werden aufgrund ihrer Wirkung als Signalstoffe als "Gasotransmitter" zusammengefasst. Diese Gase spielen eine wichtige Rolle als intra- und interzellulärer Signalstoff im Verdauungs-, Atmungs- oder Urogenitalsystem, bei der Steuerung des Herzschlags oder Nervenaktivitäten. Die Forschung ist dabei, Funktionen und weitere Details der Wirkmechanismen dieser Gase und ihre Implikationen für Physiologie, Pathophysiologie und Pharmakologie zu erarbeiten. Vom bisher neuesten Kandidaten , dem H2S , gibt es Hinweise, dass er in hoher Konzentration im Gehirn und in den Hoden vorkommt und bei Lern-/Gedächtnisprozessen sowie bei Geschlechtsfunktionen eine Rolle spielt. Durch Entwicklung von Wirksubstanzen zur Beeinflussung der H2S-Produktion oder entsprechender Zielorte könnte sich hieraus ein interessantes pharmakologisches Potenzial entwickeln. Gasotransmitters , gases as cellular signalling molecules The gases nitric oxide (NO), carbon monoxide (CO) and hydrogen sulphide (H2S) because of their capacity as signalling molecules have been now collectively termed "gasotransmitters". These gases play an important role in inter- and intracellular signalling, as in the digestive, respiratory or urogenital tract, in controlling heart activity or in nerve function. Research now tries to work out functions and further details about the mechanism of action of these gases and their implications for physiology, pathophysiology and pharmacology. The most recent candidate, H2S, is found in high concentrations in the brain and in the testis and hence is involved in learning/memory and in reproductive functions. The development of new substances interfering with the production of H2S or its targets may constitute an interesting pharmacological potential. [source] | ||||||||||||||||