PURPOSE: To obtain a bisbiguanide-based compound useful as a germicide for medical treatment, especially for operation, having a wide antimicrobial spectrum, showing excellent antibacterial activity against, Pseudomonas aeruginosa, applicable to mucosa.
CONSTITUTION: A bisbiguanide-based compound of formula I (n is 2-10) and its salt. The compound is obtained by reacting a 1,n-bis(N3-cyano-N1-gunidino)al. kane of formula II with 2 equivalent or a slightly excessive amount of 4- trifluoromethoxyaniline hydrochloride of formula III in a polar solvent and treating the prepared hydrochloride with an alkali. A germicide containing the compound is comparable to chlorhexidine (formula IV) conventionally used as a germicide in terms of width of an antibacterial spectrum, has more excellent immediate effect than chlorhexidine and further shows excellent antibacterial activity against Pseudomonas aeruginosa on which chlorhexidine has low antibacterial, action. The germicide has low irritation to mucosa and is usable in a lower concentration.
NAKAMURA AKIHIRO
HONDA TSUNETOSHI
HARADA MICHIO
TAKIZAWA MASANORI
YOSHIDA PHARM CO LTD (JP)