Abstract: The invention provides a class of water-soluble probucol derivatives having one or more ester groups replacing the phenyl hydroxyl groups of the probucol molecule. Some derivatives have polar or charged functionalities such as carboxylic acid groups, amino groups, aldehyde groups and amide groups located on the ester groups. Some of these compounds are spontaneously hydrolyzable in typical biological milieus. The present invention also provides method of treating an animal with probucol by administering a water-soluble probucol prodrug to the animal.