Synthesis and structure-activity relationships of novel antiseptics

Autor: Koichi Yasumura, Mikio Kikuchi, Kinue Ohguro, Hiroshi Ishikawa, Hidetsugu Tsubouchi
Rok vydání: 1997
Předmět:
Zdroj: Bioorganic & Medicinal Chemistry Letters. 7:1721-1724
ISSN: 0960-894X
Popis: 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 11 was chosen as a candidate novel antiseptic, which is currently under continued evaluation.
Databáze: OpenAIRE