| 2 | Author
| Nazmi Abd, Elatife Kassab, Sanaa Osman Abdallah, Hamed Abdel, Reheem Ead, Doreya Zaki | Requires 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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| default:Reihe_B/31/ZNB-1976-31b-0376.pdf | | | Identifier
| ZNB-1976-31b-0376 | | | Volume
| 31 | |
3 | Author
| F. I. Abdel-Hay, M. A. Omara, A. A. El-Barbary, M. El-Badawi | Requires 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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| default:Reihe_B/34/ZNB-1979-34b-0297.pdf | | | Identifier
| ZNB-1979-34b-0297 | | | Volume
| 34 | |
4 | Author
| Hans Moser, Grety Rihs, Hanspeter Sauter, Entwicklung Forschung, Pflanzenschutz | Requires 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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| default:Reihe_B/37/ZNB-1982-37b-0451.pdf | | | Identifier
| ZNB-1982-37b-0451 | | | Volume
| 37 | |
6 | Author
| R. Tacke, M. Strecker, W. S. Sheldrick, E. Heeg, B. Berndt, K. M. Knapstein | Requires 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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| default:Reihe_B/34/ZNB-1979-34b-1279.pdf | | | Identifier
| ZNB-1979-34b-1279 | | | Volume
| 34 | |
7 | Author
| Dagmar Denklau, Wolfgang Köhnlein, G. Erd Lüders, Joachim Steilmach | Requires 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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| default:Reihe_C/38/ZNC-1983-38c-0939.pdf | | | Identifier
| ZNC-1983-38c-0939 | | | Volume
| 38 | |
8 | Author
| Frank Beise, Harald Labischinski, Hans Bradaczek | Requires 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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| default:Reihe_C/43/ZNC-1988-43c-0656.pdf | | | Identifier
| ZNC-1988-43c-0656 | | | Volume
| 43 | |
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