1980 Volume 28 Issue 1 Pages 73-79
Pertussis, or whooping cough, has been reported to be increased with the decreased rate of pertussis vaccination. Antibacterial activities of β-lactams against both Bordetella pertussis (B. pertussis) and Haemophilus influenzae (H. influenzae) were restricted to ampicillin (ABPC) and its derivatives. Recently, β-lactams including an oxa-cephem have been developed, and found to be more active against H. influenzae than ABPC.
Assuming that β-lactams with high anti-H. influenzae activities have high activities against B. pertussis, minimum inhibitory concentrations (MICs) against 23 strains of B. pertussis isolated from the patients with whooping cough were determined by the agar dilution method, using “BORDET-GENGOU broth” as the inoculum and BORDET-GENGOU agar in which one of the twenty-five antimicrobial agents was incorporated, that was established in this study. The inoculum size had almost no effect on MICs of antimicrobials against B. pertussis except for piperacillin (PIPC).
In vitro activities of piperazine β-lactams (PIPC, T-1551) against B. pertussis were much superior to the other antimicrobial agents. Anti-B. pertussis activity of penicillins examined in this experiment was in the order:
PIPC (MIC:≤0.003-0.006μg/ml; inoculum size, 1 loopful of 106 cfu/ml)> ABPC> penicillin G≅Sulbenicillin>Cloxacillin
Anti-B. pertussis activity of cephalosporins including an oxa-cephem was in the order:
T-1551 (MIC: 0.006-0.013μg/ml; inoculum size, 1 loopful of 106 cfu/ml)>SCE-1365≅6059-S>Cefotaxime>Cefuroxime >Cefotiam≅Cefazolin≅Cephaloridine≅FK-749>Cephalexin
MICs of josamycin and minocycline were determined 0.05-0.2μg/ml in the former and 0.1-0.2 μg/ml in the latter as the inoculum was 1 loopful of 106 cfu/ml, which were superior to erythromycin and doxycycline, respectively.
Structure-activity relationships of β-lactams against B. pertussis have been discussed as compared with those against H. infiuenzae with the special reference to piperazine β-lactams and (syn) methoxyimino-cephalosporins. Further in vivo and clinical studies of B. pertussis infection are warrented.