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In Vivo Susceptibility of Mycobacterium Ulcerans to KRM-1648, a New Benzoxazinorifamycin, in Comparison With Rifampicin. Anti-mycobacterial Activity of KRM-1648

In Vivo Susceptibility of Mycobacterium Ulcerans to KRM-1648, a New Benzoxazinorifamycin, in Comparison With Rifampicin. Anti-mycobacterial Activity of KRM-1648

A M Dhople

Arzneimittelforschung. 2001;51(6):501-5.

PMID: 11455683

Abstract:

The antibacterial effects of a new benzoxazinorifamycin, KRM-1648 (3'-hydroxy-5'-(4-isobutyl-1-piperazinyl, CAS 129791-92-0), against Mycobacterium ulcerans were evaluated in vivo in mouse foot pads, and the results were compared against those obtained with rifampicin (rifampin, CAS 13292-46-1). When mice were fed with the drugs from the day of footpad inoculations, KRM-1648, at concentrations of 0.001% and higher, mixed in mouse food, was effective in inhibiting the growth of M. ulcerans in the foot pads, and the effects were bactericidal. Effects of KRM-1648 at 0.0005% were bacteriostatic. Similar results were obtained with rifampicin, but only at concentrations of 0.008% and above. In established infection, i.e., when M. ulcerans were growing actively in footpads, bactericidal effects were observed with KRM-1648 at concentrations of 0.002% and above; to obtain similar results with rifampicin, the minimum dose was 0.032%. Thus, the results suggest the superiority of KRM-1648 over rifampicin in the treatment of M. ulcerans infection. The possibility of using KRM-1648 in combination with other antimycobacterial agents is discussed.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP13292461-A	Rifampicin - CAS 13292-46-1		13292-46-1	Price

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