3-Benzoylacrylic acids and esters

Table V. Bacteriostatic and Fungistatic Activities for Substituted cis- and r Mw-3-Benzoylacrylic Acids and Their Methyl Esters...

The bacteriostatic activity of a series of substituted trans-3-benzoylacrylic acids has been successfully correlated by Hansch linear free energy relations involving polar and partition substituent constants. The activity-lipophilicity relations for this series closely parallel those found previously for other antibacterial agents, with an ideal lipophilic character for gram-positive cells of 6.1 and, for linear dependence, a slope of 0.7. A polar reaction constant, p, of about —0.6 to —0.7 is given. A possible mode of action for these acids and their related substituted cis- and trans-3-benzoyl acrylic acids and esters is discussed as an enzyme-inhibitor interaction. 

In this study we report a Hansch analysis of the activity of a series of substituted trans-3-benzoylacrylic acids. The bacteriostatic and fungistatic activity of several series of substituted cis- and trans-3-benzoyl-acrylic acids and their methyl esters are given. The structure—activity relations observed are discussed. 

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