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Appl Environ Microbiol. 1969 May; 17(5): 653-657
Copyright © 1969 American Society for Microbiology. All Rights Reserved.

Microbiological and Pharmacological Behavior of 7-Chlorolincomycin

Infectious Disease Service of the New England Medical Center Hospitals, Boston, Massachusetts 02111.
Department of Medicine, Tufts University School of Medicine, Boston, Massachusetts 02111.

ABSTRACT

Replacement of the 7-(R) hydroxyl group of lincomycin by a 7-chloro-substituent produced a compound with greater in vitro activity than the parent. Laboratory studies of this compound showed it to be highly active against all of the following strains of gram-positive organisms examined, including penicillinase- and nonpenicillinase-producing staphylococci, Diplococcus pneumoniae, Streptococcus viridans and Streptococcus pyogenes. The enterococci, as well as all the gram-negative organisms tested, with the exception of some strains of Haemophilus, were uniformly insensitive to this agent. The activity of 7-chlorolincomycin was not affected by serum or inoculum size. Resistance developed in a slow stepwise pattern. Peak levels of approximately 2 µg/ml were achieved in the serum of volunteers after ingestion of 150 mg either in the fasting state or after a meal. No untoward effects were noted. The antibiotic appears to be of potential value in the treatment of infections due to gram-positive organisms, with the exception of enterococcus.