scholarly journals Physicochemical Properties of Medicinal Agents. III. Partition Coefficients and Acid Dissociation Constants of N2-Substituted-N1-arylsulfonylurea-Derivatives

1974 ◽  
Vol 94 (1) ◽  
pp. 80-87 ◽  
Author(s):  
SHOZO ASADA ◽  
REIKO FUJITA ◽  
YUKARI SHIRAKURA
Keyword(s):  
Physicochemical Properties ◽  
Partition Coefficients ◽  
Dissociation Constants ◽  
Acid Dissociation ◽  
Acid Dissociation Constants

Biologically Important Physicochemical Properties of Some Cephalosporins

1992 ◽  
Vol 57 (8) ◽  
pp. 1739-1746
Author(s):  
Katarína Škvareninová ◽  
Štefan Baláž ◽  
Ernest Šturdík ◽  
Miroslav Veverka ◽  
Jana Adamcová ◽  
...  
Keyword(s):  
Physicochemical Properties ◽  
Partition Coefficients ◽  
Dissociation Constants ◽  
Transport Rate ◽  
Hydrolysis Rate ◽  
Antibacterial Effects ◽  
Oh Groups ◽  
Non Linear Equation ◽  
Cell Components ◽  
The Relationship

In the series of cephalosporin derivatives, consisting of eight 7-(R1-CH2-CO-NH)cephalosporanic acids and of seven analogical compounds with 3-acetoxymethyl replaced by 3-CH3, physicochemical properties, which are expected to play a role in their antibacterial effects (the transport rate parameters and partition coefficients in the systems 1-octanol-water and 1-octanol-buffer, dissociation constants of the 4-carboxyl group, reactivity towards L-glutathione imitating the nucleophilic groups of the cell components and hydrolysis rate parameters), were determined. Linear dependences were observed between the partition coefficients and the π-constants of the varying substituents as well as between reactivity towards SH-groups of L-glutathione and OH-groups. The relationship between the transport rate parameters and partition coefficients, both measured in buffered as well as non-buffered system, was described by a common non-linear equation.

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