Quantitative Struktur-Aktivitäts-Beziehungen für die Wachstumshemmung von Chlorella vulgaris-Suspensionen durch 4-Alkylsemicarbazide

Kramer, Claus-Rüdiger; Beck, Lothar; Arndt, H.

doi:10.1016/s0015-3796(82)80023-1

Cited by 7 publications

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“…Table also contains some other examples of eq with i = 1 and the integer values of the coefficients A and B 1 fitted to experimental dependencies of bioactivity , on lipophilicity. The concave dependencies were also fitted quite well by the parabolic equation and the bilinear equation with freely adjustable coefficients A and B (the results not shown).…”

Section: Numerical Simulations For Multi-bilayer Systemsmentioning

confidence: 99%

Modeling Kinetics of Subcellular Disposition of Chemicals

Baláž

2009

Chem. Rev.

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Section: Numerical Simulations For Multi-bilayer Systemsmentioning

confidence: 99%

Modeling Kinetics of Subcellular Disposition of Chemicals

Baláž

2009

Chem. Rev.

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“…So wurden im Arbeitskreis bisher isochemische Serien alkyl-und arylsubstituierter Hydrazin-und Harnstoffderivate [11][12][13][14][15][16][17][18][19], disubstituierter Benzole (vgl. Übersicht in [20]) und N-Heterocyclen [21,22] erfolgreich auf ihre wachstumshemmende Wirkung an autotroph kultivierten Chlorella-vulgaris-Suspensionen getestet, wobei für Verbindungen mit "unspezifischen" Substituenten (Alkyl-, Alkoxygruppen, Halogene) gesicherte lineare Beziehungen zwischen algistatischer Aktivität und Hydrophobizität nachgewiesen werden konnten.…”

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Beziehungen zwischen algistatischer Aktivität und physikalisch-chemischen Eigenschaften von 5-Amino-1-aryl-1H-tetrazolen

Schelenz¹

2000

J. prakt. Chem.

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205 5-Amino-1-aryl-1H-tetrazole verfügen mit muskelrelaxierenden und antiinflammatorischen [1,2], antiarthritischen, analgetischen und ulcustherapeutischen [3,4] sowie coccidiostatischen [5, 6] Eigenschaften über ein breites biologisches Wirkungsspektrum. Für isomere 5-Arylamino-1H-tetrazole und die unsubstituierte Leitstruktur 5-Amino-1H-tetrazol wurden darüber hinaus Abstract. A series of 20 5-amino-1-aryl-1H-tetrazoles was synthesized by diazotation of corresponding 1-amino-3-arylguanidines and tested for growth-inhibiting activity against autotrophic Chlorella vulgaris cultures. In the used tests the different algae growth was quantified by photometric measurements at 680 nm. From obtained dosage-effectivity relationships the reciprocal values of isoeffective concentrations c 50 were derived and defined as activity parameters A in QSAR (quantitative structure-activity relationship) studies. It could be shown that the algistatitic activity (log A) of the tested heterocycles strongly depends on hydrophobicity described by their octan-1-ol/water partition coefficients (log P). The calculated linear relationships between log A and log P can be significantly improved by separate treatment of meta-/paraand ortho-substituted compounds or using an indicator variable to describe the lower activity of ortho-substituted 5-amino-1-aryl-1H-tetrazoles in common regression equations. The results are discussed and compared with analogous QSAR found for earlier tested series of N-heterocycles and compounds with urea structure. Abb. 1 Über Extinktionsmessungen (E) erhaltene Wachstumskurven (a) wirkstoffbehandelter Chlorella-vulgaris-Kulturen(¿ c = 4,05×10 -3 mol l -1 , Ú c = 3,22×10 -3 mol l -1 , q c = 2,57×10 -3 mol l -1 , Î c = 2,06×10 -3 mol l -1 , p c = 1,61×10 -3 mol l -1 , + c = 1,03×10 -3 mol l -1 , c = 6,43×10 -4 mol l -1 , Kontrollkultur) und daraus resultierende Dosis-Wirkungs-Kurven (b) zur Ermittlung der Aktivitätsparameter log A 1 und log A 2 für die algistatische Wirksamkeit von 5-Amino-1-phenyl-1H-tetrazol (vgl. Text)

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Subcellular Pharmacokinetics and Drug Properties: Numerical Simulations in Multicompartment Systems

Baláž

1994

Quant. Struct.‐Act. Relat.

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The methodology and results of numerical simulations of drug distribution in multicompartment systems, represented by a catenary set of alternating aqueous and lipid compartments, are reviewed. Transport, membrane accumulation, protein binding, first order elimination (biotransformation or excretion), but not ionisation have been considered as the processes determining the drug distribution. The simulations provide the time courses of the drug concentrations in individual compartments as dependent on hydrophobicity and elimination rate parameters of drugs because the model parameters are substituted by their relationships to the drug properties. The simulation results are fitted with empirical functions, mostly in the form of the hydrophobicity‐concentration profiles for a pre‐defined time of exposure. The shape of the profiles is different for open and closed biological systems (with and without elimination, respectively) as well as for individual periods of the drug distribution in closed systems (non‐equilibrium, mixed, equilibrium). Fitting the empirical functions to experimental data enables one to verify quantitatively the simulation results. The use of the approach for formulation of mechanistic conclusions is exemplified.

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Quantitative Struktur-Aktivitäts-Beziehungen für die Wachstumshemmung von Chlorella vulgaris-Suspensionen durch 4-Alkylsemicarbazide

Cited by 7 publications

References 1 publication

Modeling Kinetics of Subcellular Disposition of Chemicals

Modeling Kinetics of Subcellular Disposition of Chemicals

Beziehungen zwischen algistatischer Aktivität und physikalisch-chemischen Eigenschaften von 5-Amino-1-aryl-1H-tetrazolen

Subcellular Pharmacokinetics and Drug Properties: Numerical Simulations in Multicompartment Systems

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