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1Author    Bernd Sorg, Michael Gschwendt, HeinzWalter Thielmann, Erich HeckerRequires cookie*
 Title    Struktur-Wirkungsbeziehungen polyfunktioneller Diterpene des Tigliantyps, IV [1-3] Structure-Activity Relationships of Polyfunctional Diterpenes of the Tigliane Type, IV [1-3] Derivatives of Tigliane without or with Opened Cyclopropane Ring and their Irritant and Promoting Activity  
 Abstract    Derivate des Tiglians mit fehlendem oder geöffnetem Cyclopropanring und ihre irritierende und tumorpromovierende Wirkung The synthesis of the esters 6d-8d, 9 c and 10 c is described. These compounds are closely structurally related to the irritant and tumorpromoting 12-0-tetradecanoylphorbol-13-acetate (TPA, 2 a) and to phorbol-12,13-didecanoate (PDD, 2 c) except that they possess no cyclopropane ring. Biological tests show that opening or complete removal of the cyclopropane ring leads to nearly total loss of irritant or tumorpromoting (tested in the case of 9 c and 10 c) activity. 
  Reference    Z. Naturforsch. 35b, 1470—1475 (1980); eingegangen am 2. Juni 1980 
  Published    1980 
  Keywords    Cocarcinogens, Phorbol, Structure-activity-relationship, Tumor Promoter, Irritants 
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 TEI-XML for    default:Reihe_B/35/ZNB-1980-35b-1470.pdf 
 Identifier    ZNB-1980-35b-1470 
 Volume    35 
2Author    Alfred Gieren, Michail KokkinidisRequires cookie*
 Title    Structure Investigations o f Agonists o f the Natural Neurotransmitter Acetylcholine II [1| X-ray Structure Analysis o f Trimethyl(4-oxopentyl)ammonium-chloride  
 Abstract    The crystal structure of Trimethyl(4-oxopentyl)ammonium-chloride ([(C H 3) 3 N —(CH^aCOCHjJCl-) (1) was determined by an X-ray structure analysis. 1 crystallizes in the orthorhombic space group P21 21 21 with a = 10.440 (3), b = 14.600 (9), c = 6.804 (9) A and with four formula units per unit cell. The structure was solved by a Patterson and a successive Fourier synthesis. The least squares refinement yielded an R-value o f 0.064 for 1077 observed reflections. The cation o f 1 is derived from acetylcholine by replacement o f the ester oxygen with a CH2 group. It shows a potent nicotinic activity and a significant difference in conformation as compared with acetylcholine. In the crystal structure the anions are oriented stereospecifically with respect to the tetrahedron of the quaternary ammonium group. The geometry o f two triangles formed by the quaternary nitrogen atom, the oxygen atom o f the carbonyl group, and by either o f the two anions nearest to the quaternary ammonium group is characteristic for the nicotinic activity o f 1. 
  Reference    Z. Naturforsch. 37c, 282 (1982); received December 231981 
  Published    1982 
  Keywords    X-ray, Neurotransmitter, Cation-Anion Interactions, Structure-Activity Relationships 
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 TEI-XML for    default:Reihe_C/37/ZNC-1982-37c-0282.pdf 
 Identifier    ZNC-1982-37c-0282 
 Volume    37 
3Author    Berg, M. Arjo, Brandse Duphar, B. V. BiochemistryRequires cookie*
 Title    G erard van den  
 Abstract    The effects of the algicide PH 40-62 on photosynthetic reactions in spinach chloroplasts were studied. The compound proved to be an uncoupler o f photophosphorylation, whereas inhibition of photosynthetic electron transport occurred at higher concentrations. The site of this inhibition was before photosystem II. The uncoupling effect was partially reversible. In a series o f related compounds the uncoupling activity appeared mainly dependent on the lipophilic properties o f the compounds but electronic effects also played a distinct role. C om paring these uncoupling data with those of some known series of uncouplers it appeared that lipophilicity determ ines the uncoupling activity in an identical way and a regression equation was found describing the uncoupling activities of 60 compounds belonging to four chemically different groups of com ­ pounds. 
  Reference    Z. Naturforsch. 39c, 107—114 (1984); received Septem ber 19 1983 
  Published    1984 
  Keywords    Arylethanediamines, Photophosphorylation, U ncouplers, Structure-Activity Relationships 
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 TEI-XML for    default:Reihe_C/39/ZNC-1984-39c-0107.pdf 
 Identifier    ZNC-1984-39c-0107 
 Volume    39 
4Author    HermannL. LotterRequires cookie*
 Title    Untersuchung der Struktur-Wirkungsbeziehung antihepatotoxischer Naturstoffe (Silybin-Antamanid) durch Röntgenstrukturanalyse  
 Abstract    Both, the flavonolignane silybin and the decapeptide antam anide, protect anim als against the mushroom poison phalloidin from Amanita species. The X-ray structures o f silybin and anta­ manide have been solved in previous studies. Here an attempt has been m ade to explain the antagonistic antihepatotoxic protection by sim ilar chem ical structure elem ents in the two compounds. It can be shown that two aromatic rings in a definite arrangement are essential for the attachment to the target structure o f the liver cell membrane. Com parable pharm acological tests are discussed. 
  Reference    Z. Naturforsch. 39c, 535 (1984); received Decem ber 2 1983/March 26 1984 
  Published    1984 
  Keywords    Silybin, Antamanide, Phalloidin, Structure Activity Relationship, A ntihepatotoxic Principle 
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 TEI-XML for    default:Reihe_C/39/ZNC-1984-39c-0535.pdf 
 Identifier    ZNC-1984-39c-0535 
 Volume    39 
5Author    K. Öm Ívesa, K. Riton, K. HatziosbRequires cookie*
 Title    Chemistry and Structure-Activity Relationships of Herbicide Safeners  
 Abstract    The discovery and commercial success of safeners against thiolcarbamate herbicide injury to corn has stimulated a rapid progress and opened new possibilities for further research and development in the last decade. Compounds with new chemistry, increased efficacy, and a broader selectivity spectrum were synthesized and developed for agricultural use. Structure-activity relationship studies helped to optimize their chemical properties and to understand their biological modes of action. Several examples indicate close similarity between chemical structures possessing herbicidal and safener properties. In some cases this differentiation may be marginal, as shown in crops pretreated with low herbicide doses leading to safening effects. In other examples, however, structural optima for safening and herbicidal efficacy can be clearly differentiated. 
  Reference    Z. Naturforsch. 46c, 798—804 (1991); received March 26 1991 
  Published    1991 
  Keywords    Safeners, Chemical Properties, Structure-Activity Relationships 
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 TEI-XML for    default:Reihe_C/46/ZNC-1991-46c-0798.pdf 
 Identifier    ZNC-1991-46c-0798 
 Volume    46 
6Author    HerbertOliver Kolodziej3, HermanJ. Kayser3, Wim Woerdenbagb, Niesko Van Udenb, PrasRequires cookie*
 Title    Structure -Cytotoxicity Relationships of a Series of Natural and Semi-Synthetic Simple Coumarins as Assessed in Two Human Tumour Cell Lines  
 Abstract    The cytotoxicity of 22 natural and semi-synthetic simple coumarins was evaluated in G LC4, a human small cell lung carcinoma cell line, and in CO LO 320. a human colorectal cancer cell line, using the microculture tetrazolium (MTT) assay. With IC 50 values > 100 j.i m , following a continuous (96h) incubation, most coumarins exhibited only low cytotoxicity. Several com­ pounds, however, displayed significant potencies. As far as the structure -cytotoxicity rela­ tionship is concerned, it is conspicuous that all the potentially active natural compounds possess at least two phenolic groups in either the 6,7-or 6,8-positions. In addition, the 5-formyl-6-hydroxy substituted semi-synthetic analogue was found to be potent, reflecting the importance of at least two polar functions for high cytotoxicity. 
  Reference    Z. Naturforsch. 52c, 240—244 (1997); received November ll/December 5 1996 
  Published    1997 
  Keywords    Coumarins, Cytotoxicity, Structure-Activity Relationships, Pelargonium sidoides, Geraniaceae 
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 TEI-XML for    default:Reihe_C/52/ZNC-1997-52c-0240.pdf 
 Identifier    ZNC-1997-52c-0240 
 Volume    52 
7Author    Oliver Kayser, H. Erbert KolodziejRequires cookie*
 Title    Antibacterial Activity of Simple Coumarins: Structural Requirements for Biological Activity  
 Abstract    The antibacterial activity of a series of simple coumarins was evaluated against 8 microor­ ganisms, including three Gram-positive (Staphylococcus aureus, beta-hemolytic Streptococcus and Streptococcus pneum oniae) and five Gram-negative bacteria (Escherichia coli, Klebsiella pneum oniae, Pseudom onas aeruginosa, Proteus mirabilis and H aemophilus influenzae), using the microdilution broth method. The coumarins tested showed broad diversity regarding growth inhibitory activity with minimum inhibitory concentrations ranging from 0.9 to >12.4 (j.M . This study, presenting the first systematic analysis of structure-activity relationships among this group of coumarins, revealed some interesting structural requirements. While coumarins with a methoxy function at C-7 and, if present, an OH group at either the C-6 or C-8 position are invariably effective against the spectrum of tested standard bacteria (Gram-negative microorganisms including the Gram-positive bacterium Staphylococcus aureus), the presence of an aromatic dimethoxy arrangement is apparently favourable against those mi­ croorganisms which require special growth factors (beta-hemolytic Streptococcus, Streptococ­ cus pneum oniae and Haem ophilus influenzae). A combination of these structural features, two methoxy functions and at least one additional phenolic group as reflected by the highly oxygenated coumarins, identify promising candidates with antibacterial broad-spectrum ac­ tivity. 
  Reference    Z. Naturforsch. 54c, 169—174 (1999); received November 11/December 8 1998 
  Published    1999 
  Keywords    Coumarins, Antibacterial Activity, Structure-Activity Relationships 
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 TEI-XML for    default:Reihe_C/54/ZNC-1999-54c-0169.pdf 
 Identifier    ZNC-1999-54c-0169 
 Volume    54 
8Author    Ernst Priesner, Hans-Jürgen Bestmann, Otto Vostrowsky, Peter RöselRequires cookie*
 Title    Sensory Efficacy of Alkyl-Branched Pheromone Analogues in Noctuid and Tortricid Lepidoptera  
 Abstract    The effect of introducing alkyl substituents (methyl to pentyl) to the chain segment n in long-chain alkenyl acetates, CH3(CH2)nCH = CH(CH2) O T -0-C0CH3 (I), was investigated in pheromone receptors of Noctuidae, Tortricidae, and Cochylidae species. The receptor types studied were maximally responsive to (Z)-7-or (Z)-9-dodecen-l-yl acetate, (Z)-l-, (Z)-9-, or (Z)-11-tetradecen-1-yl acetate, or (Z)-11-hexadecen-l-yl acetate, representing key compounds with re = l, n = 3, or n = 5 methylene groups. In terms of the relative stimulus amounts required to elicit equivalent EAG amplitudes, the efficacy of the alkyl-branched derivatives was between 1/1000 to 300 times that of the unbranched chain of the same length and double bond position. The effects of branching were specific to the type of receptor, the length and double bond position of the parent chain, and the kind and position of the alkyl substituent. The most pronounced increase observed occurred with receptors for « = 1 type pheromones, (Z)-9-dodecen-l-yl acetate and (Z) -11-tetradecen-l-yl acetate when an a-methyl group was introduced to elongated derivatives; whereas the greatest decreasing effects were obtained on receptors for the n = 5 type compound, (Z)-7-tetradecen-l-yl acetate. The results show basic differences in structure-response relationships between the Noctuidae vs Tortricidae receptors studied. Various possible effects of the substituent groups during sensory transduction are considered. The data should contribute to further elucidation of interaction mechanisms of unbranched alkenyl acetate pheromones (I) with insect olfactory receptors. 
  Reference    (Z. Naturforsch. 32c, 979 [1977]; received August 15 1977) 
  Published    1977 
  Keywords    Pheromones, Alkenyl Acetates, Olfactory Receptors, Structure-Activity Relationships, Lepidoptera 
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 TEI-XML for    default:Reihe_C/32/ZNC-1977-32c-0979.pdf 
 Identifier    ZNC-1977-32c-0979 
 Volume    32 
9Author    R. Tacke, A. Bentlage, W. S. Sheldrick, L. Ernst, K. StoepelRequires cookie*
 Title    Sila-Pharmaka, 24. Mitt. [1] Sila-Analoga von Nifedipin-ähnlichen 4-Aryl-2.6-cümethyl-1.4-dihydropyridin- 3.5-dicarbonsäure-dialkylestern, II Sila-Drugs, 24 th Communication [1] Sila-Analogues of Nifedipine-Like Di alkyl 4-Aryl-2,6-dimethyl-l,4-dihydropyridine- 3,5-dicarboxylates, II  
 Abstract    In the course of systematic studies on sila-substituted drugs the nifedipine-like 1.4-di-hydropyridine derivatives 4 a, 4 b and 4 c were prepared and investigated with respect to sila-substitution effects. By X-ray diffraction analyses 4 a, 4 b and 4 c were found to be isostructural. The C/Si-analogues exhibit similar spasmolytic activities (in vitro, guinea pig ileum), comparable with that of nifedipine. However, the compounds differ sub-stantially in their in vivo activity, as measured by the antihypertensive effect on the renal-hypertensive rat. The experimental results are discussed with respect to the carbon/silicon exchange. 
  Reference    Z. Naturforsch. 37b, 443—450 (1982); eingegangen am 25. September 1981 
  Published    1982 
  Keywords    Sila-Analogues of Nifedipine Derivatives, X-ray, Pharmacological Activity, Structure-Activity Relationships 
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 TEI-XML for    default:Reihe_B/37/ZNB-1982-37b-0443.pdf 
 Identifier    ZNB-1982-37b-0443 
 Volume    37 
10Author    Reinhold Tacke, Haryanto Linoh, MoayadT. Attar-Bashi, WilliamS. Sheldrick, Ludger Ernst, Roland Niedner, Joachim FrohneckeRequires cookie*
 Title    Sila-Pharmaka, 26. Mitt. [1] Darstellung und Eigenschaften potentiell curarewirksamer Silicium-Verbindungen, III Sila-Pharmaca, 26th Communication [1] Preparation and Properties of Silicon Compounds with Potential Curare-Like Activity, III  
 Abstract    The potentially curare-hke silicon compounds 8a-Sf were synthesized and investigated with respect to their structure-activity relationships. The conformations of the com-pounds in the solid state and in solution were studied by X-ray diffraction analysis (8a-8e) and *H NMR spectroscopy (8a-8f), respectively. The muscle relaxing properties of 8a-8f were investigated on the mouse. The observed structure-activity relationships are not in accordance with the classical "14 A model" for neuromuscular blocking agents. Einführung 
  Reference    Z. Naturforsch. 37b, 1461—1471 (1982); eingegangen am 19. April 1982 
  Published    1982 
  Keywords    Silicon Compounds, Curare-Like Activity, X-ray, Conformational Analyses, Structure-Activity Relationships 
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 TEI-XML for    default:Reihe_B/37/ZNB-1982-37b-1461.pdf 
 Identifier    ZNB-1982-37b-1461 
 Volume    37 
11Author    Harald Labischinski, Dieter Naumann, Gerhard Barnickel, Wolfgang Dreißig, Wojciech Gruszecki, Andreas Hofer, Hans BradaczekRequires cookie*
 Title    Comparison between the Molecular and Crystal Structures of a Benzylpenicillin Ester and its Corresponding Sulfoxide with Drastically Reduced Biological Activity  
 Abstract    A comparative X-ray structure determination was performed to elucidate possible conforma-tional differences between penicillins and penicillin sulfoxides. Penicillin-G-acetoxy-methylester and its Iß-oxide were used as model substances, because the only chemical difference between both compounds resides in the thiazolidine ring sulfur oxidation. On the basis of the X-ray data as well as of infrared measurements it is discussed that the drastically reduced biological activity of the penicillin-G-sulfoxide might be related to conformational differences in thiazolidine ring puckering or, even more simply, to the geometric position of the sulfoxide oxygen atom, both of which may hamper the proper reaction of the sulfoxide with its target enzyme(s). 
  Reference    Z. Naturforsch. 42b, 367—375 (1987); received June 30/0ctober 14 1986 
  Published    1987 
  Keywords    X-Ray, Penicillin G, Penicillin G Sulfoxide, Thiazolidine Ring Conformation, Structure Activity Relationships 
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 TEI-XML for    default:Reihe_B/42/ZNB-1987-42b-0367.pdf 
 Identifier    ZNB-1987-42b-0367 
 Volume    42 
12Author    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