Synthesis and structure-activity relationships of novel antiseptics

Article abstract of DOI:10.1016/S0960-894X(97)00297-7

For the purpose of developing new antiseptics, we searched for compounds having high biocidal activity covering both gram-positive and gram-negative bacteria. Accordingly, we designed 1,5-disubstituted biguanides and synthesized them using two alternative efficient reaction schemes. The bactericidal activity of these biguanides was assayed by the micro titration plate method. Among the biguanides synthesized, 3,4-dichlorobenzyl derivatives were found to exhibit particularly high bactericidal activity. Ultimately, compound II was chosen as a candidate novel antiseptic, which is currently under continued evaluation.