Activity of lipid-soluble inhibitors of dihydrofolate reductase against Pneumocystis carinii in culture and in a rat model of infection

S. F. Queener, M. S. Bartlett, M. A. Jay, M. M. Durkin, J. W. Smith

Research output: Contribution to journalArticle

57 Scopus citations

Abstract

Trimetrexate and BW301U (piritrexim isethionate), lipid-soluble inhibitors of dihydrofolate reductase, are potent inhibitors of the growth of Pneumocystis carinii in culture with WI-38 cells. Inhibition was observed with 0.1 μg of trimetrexate or BW301U per ml. Trimethoprim is ineffective at 100 μg/ml in this culture system. Both trimetrexate and BW301U were effective as prophylactic agents against P. carinii pneumonia in rats; trimetrexate at 7.5 mg/kg protected 9 of 10 rats, and BW301U at 5 mg/kg protected 4 of 10.

Original languageEnglish (US)
Pages (from-to)1323-1327
Number of pages5
JournalAntimicrobial Agents and Chemotherapy
Volume31
Issue number9
DOIs
StatePublished - Jan 1 1987

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)
  • Infectious Diseases

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