Semisynthetic Penicillin 6-[ d (—)-α-Carboxy-3-Thienylacetamido] Penicillanic Acid Active Against Pseudomonas In Vitro

Abstract

The activity of 6-[ d (—)-α-carboxy-3-thienylacetamido] penicillanic acid, BRL2288, was determined against Pseudomonas aeruginosa and various gram-negative bacilli. The majority of Pseudomonas strains (89%) were inhibited by 100 μg of the antibiotic per ml. BRL2288 is twofold more active than carbenicillin against Pseudomonas at 100 μg/ml or less. Among Enterobacteriaceae tested, 87% Enterobacter and 87% of Proteus mirabilis strains were inhibited by 25 μg/ml or less. Indole-positive Proteus were inhibited by 10 μg/ml or less. Fifty-five per cent of ampicillin-resistant Escherichia coli were inhibited by 100 μg/ml. Klebsiella were uniformly resistant. BRL2288 is not hydrolyzed by most resistant Pseudomonas , but it is destroyed by the β-lactamases of E. coli and P. mirabilis. The antibiotic shows synergy with gentamicin but not with penicillinase-resistant penicillins such as cloxacillin. Activity of BRL2288 against gram-positive organisms is two- to eightfold less than that of ampicillin or benzylpenicillin G.