Zur Toxicit�t des Sulfaphenylpyrazols

Seydel, Joachim K.; Wolter, Hans; Krueger-Thiemer, E; Wempe, E

doi:10.1007/bf01478099

Cited by 6 publications

(1 citation statement)

References 3 publications

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“…This, in fact, has been observed. 41 Quantitative Structure-Activity Relationships (QSAR). If we assume that the liberation of INA by the oxidizing system is not rate determining in analogue formation and if we limit our studies to INH-sensitive strains (with complete oxidizing enzyme system), the biological activity of INH derivatives should depend on the reactivity of the pyridine nitrogen atom (the possible disturbance of the functions of the bacterial peroxidase in response to different substituents is presently being investigated and will be published elsewhere).…”

Section: II Iiimentioning

confidence: 99%

Mode of action and quantitative structure-activity correlations of tuberculostatic drugs of the isonicotinic acid hydrazide type

Seydel¹,

Schaper²,

Wempe³

et al. 1976

J. Med. Chem.

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Quantitative structure-activity studies have been performed for a series of 2-substituted isonicotinic acid hydrazides by correlating electronic, steric, and lipophilic properties of the substituents with the biological activity date (MIC) from serial dilution tests with Mycobacterium tuberculosis (strain H 37 Rv). The reaction rates for the quaternization of 2-substituted pyridines with methyl iodide were also determined. The rate constants show a similar dependence on the steric and electronic effects of the substituents as the antibacterial activities of the corresponding pyridine-4-carboxylic acid hydrazides. The obtained correlations give evidence that the reactivity of the pyridine nitrogen atom is essential for the biological activity of 2-substituted isonicotinic acid hydrazides and seem to support the hypothesis that isonicotinic acid derivatives are incorporated into an NAD analogue.

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Section: II Iiimentioning

confidence: 99%

Mode of action and quantitative structure-activity correlations of tuberculostatic drugs of the isonicotinic acid hydrazide type

Seydel¹,

Schaper²,

Wempe³

et al. 1976

J. Med. Chem.

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Zur Methylierung von 1‐Phenyl‐5‐sulfanilamido‐pyrazol

Eichenberger

Zürcher

Rossi

et al. 1965

Helvetica Chimica Acta

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wurden in 400 ml Feinsprit rnit 900 mg Rum-Nickel als Katnlysator hydriert. Nach Aufnahme der berechneten Menge (336 ml H,) wurde unterbrochen und der Katalysator abfiltriert. Den Katalysator kochte man nochmals mit 350 ml Athanol aus, vereinigte die beiden alkoholischen Filtrate uncl dampfte zur Trockne ein. Den Riickstand, 0.85 g, lrristallisierte man aus Alkohol um: 0,55g vom Smp. 211-215". Eine nochmals zur Analyse umBristallisicrteProbe schniolz bei 212-215".

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