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'Structure Activity Relationship' in keywords Facet   section ZfN Section B  [X]
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1987 (1)
1982 (2)
1980 (1)
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    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 
3Author    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 
4Author    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