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1Author    AngelM. RelimpioRequires cookie*
 Title    Structure and Anticholinesterase Activity of Series of Ethyl Substituted Phenyl Methylphosphonates  
 Abstract    Thirty derivates from substituted-phenyl-ethyl methylphosphonates have been synthesized and their inhibiting power of acetyl-cholinesterase have been examined in vitro and in vivo. The cor­ relation between inhibition of the enzyme and electrophylic power of the substituent of the phenyl group was excellent, but when this group contains two substituents, steric factors appear to operate. The activity of these compounds has been demonstrated to be higher than their phosphate analogs. 
  Reference    (Z. Naturforsch. 32c, 760 [1977]; received June 13 1977) 
  Published    1977 
  Keywords    Cholinesterase, Methylphosphonates, Inhibitors, Biological Activity 
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 TEI-XML for    default:Reihe_C/32/ZNC-1977-32c-0760.pdf 
 Identifier    ZNC-1977-32c-0760 
 Volume    32 
2Author    Nazmi Abd, Elatife Kassab, Sanaa Osman Abdallah, Hamed Abdel, Reheem Ead, Doreya ZakiRequires cookie*
 Title    Some New Tetrahydrothiopyrano[2,3-d]thiazole-2-thione Derivatives and their Biological Activities 3-Phenyl-2,4  
  Reference    (Z. Naturforsch. 31b, 376—379 [1976]; received August 14 1975) 
  Published    1976 
  Keywords    thiazolidinedithiones, 1, 4-Cycloaddition, Heterodienes, Synthesis, Biological Activities 
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 TEI-XML for    default:Reihe_B/31/ZNB-1976-31b-0376.pdf 
 Identifier    ZNB-1976-31b-0376 
 Volume    31 
3Author    F. I. Abdel-Hay, M. A. Omara, A. A. El-Barbary, M. El-BadawiRequires cookie*
 Title    Organophosphorus Compounds of Expected Biological Activity, Part II* Preparation of Thiourea Derivatives and N-Aryl-phosphorothiomonoamidates  
 Abstract    The examples of cyclodiphosphazanes so far studied do not contain any nuclei of biological interest [1]. In the present investigation we aimed to introduce ethyl p-amino-benzoate, 2-aminopyridine residues in the phosphazane molecule. For this purpose phos-phorus pentachloride was treated with ethyl p-aminobenzoate, p-anisidine, 2-amino-pyridine and 5-aminoquinoline to give l,3-di-j9-ethoxycarbonylphenyl-, l,3-di-j9-methoxy-phenyl-, l,3-di-2-pyridyl-and l,3-di-5-quinolinyl-2,2,2,4,4,4-hexachlorocyclo-diphos-phazane (la-d), respectively. The compounds la-d were treated with potassium thio-cyanate in acetone. The oily products formed were then treated with p-anisidine, ethyl-p-aminobenzoate and 2-aminopyridine whereupon solid products (2a-h) were obtained. The reaction probably takes place according to the following mechanism [2]. la: b: c: d: Ar 1 Ar C2H5OOCC6H4-(p) CH3OC6H4-(p) C5H4N-(2) C9H6N-(5) Ar Cl /N Cl ci >0< ci SCN NCS 2a: b: c: 
  Reference    Z. Naturforsch. 34b, 297—299 (1979); received October 16 1978 
  Published    1979 
  Keywords    Organophosphorus Compounds, Thiourea Derivatives, Biological Activity 
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 TEI-XML for    default:Reihe_B/34/ZNB-1979-34b-0297.pdf 
 Identifier    ZNB-1979-34b-0297 
 Volume    34 
4Author    Hans Moser, Grety Rihs, Hanspeter Sauter, Entwicklung Forschung, PflanzenschutzRequires cookie*
 Title    Der Einfluß yon Atropisomerie und chiralem Zentrum auf die biologische Aktivität des Metolachlor The Influence of Atropisomerism and Chiral Centre on the Biological Activity of Metolachlor  
 Abstract    The four stereoisomers of the grass herbicide Metolachlor, the isomerism of which is based on a combination of a chiral centre and a chiral axis, were prepared, and their absolute configurations determined by X-ray analysis. The synthesis was achieved by using optically active starting materials and new optically active carbamates as intermediates. The herbicidal activity is mainly influenced by the chiral centre, the S-isomers being the most active ones. 
  Reference    Z. Naturforsch. 37b, 451—462 (1982); eingegangen am 20. August 1981 
  Published    1982 
  Keywords    Chloro-acetanilide, Metolachlor, Atropisomerism, Chiral Centre, Biological Activity 
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 TEI-XML for    default:Reihe_B/37/ZNB-1982-37b-0451.pdf 
 Identifier    ZNB-1982-37b-0451 
 Volume    37 
5Author    Irene UrbaschRequires cookie*
 Title    Transformationen von trans-2-Hexenal durch Botrytis cinerea PERS. als Entgiftungsmechanismen Transformations of trans-2-H exenal by Botrytis cinerea PERS. as Detoxification M echanisms  
 Abstract    The m etabolization of /rö«5-2-hexenal — one of the main components of plant wound gases with antibiotic activity — was investigated for 5 different isolates of Botrytis cinerea PERS. The transform ation products as well as the kinetics of their formation were analyzed. Isolates exclusively mycelium forming (Be 1 and Be 13) transform ed rr-2-hexenal into tr-2-hexenol, while sporulating isolates (Be 3, Be 9 and Be 10) converted rr-2-hexenal to hexanol-1. Basically the m etabolization of rr-2-hexenal proceeded in the same way via the aqueous phase as in the gas phase. The transform ation products fr-2-hexenol and hexanol-1 showed significantly lower toxicity against the tested B. cinerea isolates than ?/--2-hexenal. In each isolate the end product of tr-2-hexenal conversion had the weakest inhibitory activity. The transform ation reactions thus repre­ sent detoxification mechanisms for these fungi. 
  Reference    Z. Naturforsch. 42c, 64—68 (1987); received August 26/November 12 1986 
  Published    1987 
  Keywords    Botrytis cinerea, fr-2-Hexenal Conversion, Biological Activity, Detoxification 
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 TEI-XML for    default:Reihe_C/42/ZNC-1987-42c-0064.pdf 
 Identifier    ZNC-1987-42c-0064 
 Volume    42 
6Author    R. Tacke, M. Strecker, W. S. Sheldrick, E. Heeg, B. Berndt, K. M. KnapsteinRequires cookie*
 Title    Sila-Pharmaka, 14. Mitt. [1] Darstellung und Eigenschaften sowie Kristall-und Molekülstruktur von Sila-Difenidol Sila-Drugs, 14 th Communication [1] Preparation and Properties as well as Crystal and Molecular Structure of Sila-Difenidol  
 Abstract    Sila-difenidol (6 b), a sila-analogue of the drug difenidol (6 a), was synthesized according to Scheme 1. 6 b and its new precursors 3 and 5 were characterized by their physical and chemical properties, and their structures confirmed by elementary analyses, *H NMR and mass spectroscopy. 6 b crystallizes orthorhombic P 2i 2i 2i with a — 11.523(1), b = 14.366(4), c = 11.450(1) A, Z = 4, Dber = 1.14 gcm-3. The structure was refined to fi = 0.050 for 1897 reflexions. A strong nearly linear intramolecular 0-H---N hydrogen bond of 2.685 A is observed. The anticholinergic, histaminolytic and musculotropic spasmolytic activities of 6 a and 6 b are reported. 
  Reference    Z. Naturforsch. 34b, 1279—1285 (1979); eingegangen am 16. März 1979 
  Published    1979 
  Keywords    Sila-Difenidol, Syntheses, Crystal Structure, Molecular Structure, Biological Activity 
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 TEI-XML for    default:Reihe_B/34/ZNB-1979-34b-1279.pdf 
 Identifier    ZNB-1979-34b-1279 
 Volume    34 
7Author    Dagmar Denklau, Wolfgang Köhnlein, G. Erd Lüders, Joachim SteilmachRequires cookie*
 Title    Isolation and Fast Purification o f Neocarzinostatin by FPLC-Ion Exchange Chromatography  
 Abstract    Neocarzinostatin, a highly toxic antitum or protein containing an essential nonprotein Chromo­ phore, can be isolated and purified from culture filtrates o f Streptomyces carzinostaticus. Usually a lengthy procedure of up to 60 h is necessary for the isolation, including several chromatographic steps partly under conditions which favour inactivation of the drug by release of chrom ophore. We describe a new method yielding practically clinical grade N eocarzinostatin from crude extracts in 20 min. This very fast and reproducible m ethod was m ade possible by using a Mono Q anion exchange column filled with m onodisperse gel m aterial which has been recently developed. 
  Reference    Z. Naturforsch. 38c, 939 (1983); received July 1/August 31 1983 
  Published    1983 
  Keywords    Zinostatin, Antitumor Antibiotic, Fast Purification, Biological Activity, Protein-H PLC 
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 TEI-XML for    default:Reihe_C/38/ZNC-1983-38c-0939.pdf 
 Identifier    ZNC-1983-38c-0939 
 Volume    38 
8Author    Frank Beise, Harald Labischinski, Hans BradaczekRequires cookie*
 Title    On the Relationships between Molecular Conformation, Affinity towards Penicillin-Binding Proteins, and Biological Activity of Penicillin G-Sulfoxide  
 Abstract    The binding capacity of penicillin G-sulfoxide towards the penicillin-binding proteins (PBP) of Staphylococcus aureus H was studied. The sulfoxide and its parent compound, penicillin G, differ only in two aspects, the sulfur-bound oxygen and an altered conformation of the five-membered thiazolidine-ring system. These minor alterations of the penicillin structure resulted in a drastical decrease of binding activity (about two orders of magnitude) of the sulfoxide derivative towards its target enzymes. Furthermore, the sulfoxide did not exhibit the selectivity of subinhibitory doses for PBP 3, as could be observed for penicillin G. The biological consequences of this behaviour were monitored via growth curves, uptake of cell wall label, and analysis of the cell wall. Binding studies revealed that comparable growth inhibi-tion and impairment of cell wall label uptake were achieved by at least a 100-fold higher penicillin G-sulfoxide concentration, compared to its parent compound. In cell wall analysis, the application of high doses of the antibiotics, i.e. nearly saturated PBP, verified the above mentioned observation. Surprisingly, small but significant differences in cell wall composition occurred using subinhibitory doses, probably due to the altered affinity towards PBP 3, supporting the hypothesis of an important role of this PBP in peptidoglycan transpeptida-tion. 
  Reference    Z. Naturforsch. 43c, 656—664 (1988); received March 25/June 28 1988 
  Published    1988 
  Keywords    Penicillin G, Penicillin G-Sulfoxide, Penicillin-Binding Proteins, Biological Activity, Structure Activity Relationships 
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 TEI-XML for    default:Reihe_C/43/ZNC-1988-43c-0656.pdf 
 Identifier    ZNC-1988-43c-0656 
 Volume    43