| | 1 | Author
| Bernd Sorg, Michael Gschwendt, HeinzWalter Thielmann, Erich Hecker | Requires 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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| default:Reihe_B/35/ZNB-1980-35b-1470.pdf | | | | Identifier
| ZNB-1980-35b-1470 | | | | Volume
| 35 | |
| 2 | Author
| R. Tacke, A. Bentlage, W. S. Sheldrick, L. Ernst, K. Stoepel | Requires 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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| default:Reihe_B/37/ZNB-1982-37b-0443.pdf | | | | Identifier
| ZNB-1982-37b-0443 | | | | Volume
| 37 | |
| 3 | Author
| Reinhold Tacke, Haryanto Linoh, MoayadT. Attar-Bashi, WilliamS. Sheldrick, Ludger Ernst, Roland Niedner, Joachim Frohnecke | Requires 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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| default:Reihe_B/37/ZNB-1982-37b-1461.pdf | | | | Identifier
| ZNB-1982-37b-1461 | | | | Volume
| 37 | |
| 4 | Author
| Harald Labischinski, Dieter Naumann, Gerhard Barnickel, Wolfgang Dreißig, Wojciech Gruszecki, Andreas Hofer, Hans Bradaczek | Requires 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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| default:Reihe_B/42/ZNB-1987-42b-0367.pdf | | | | Identifier
| ZNB-1987-42b-0367 | | | | Volume
| 42 | |
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