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'Structure activity relationship' in keywords Facet   Publication Year 1982  [X]
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1Author    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 
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