The Effect of Ring Size on the Biological Activity of Nitrogen Containing Compounds

Abstract

The biological activity of N-containing ring compounds was studied as a function of the distribution coefficient of these compounds in 1-octanol/water system. The reaction used to monitor activity is the detritiation of 3[H]- acetophenone in dimethylsulfoxide affected by the nitrogen bases understudy at 25.0oC A strong correlation was found between the rate of detretiation of labeled acetophenone and the basicity of N-containing ring cyclic compounds. The correlation coefficient and regression constant were 1.0321 and R2= 0.9415 respectively. This finding shows that similar factors were involved in both cases. Whenever these bases are part of the structure of a drug e.g., they may cause deprotonation of some alkyl groups e.g an acyl hence altering its distribution and binding to the receptor.

Keywords

• Detritiation, Partition Coefficient, TLC, DMSO