8-Aminoquinolines from Walter Reed Army Institute for Research for treatment and prophylaxis of Pneumocystis pneumonia in rat models.

Abstract

Three 8-aminoquinolines from the Walter Reed Army Institute for Research (WRAIR), WR6026, WR238605, and WR242511, strongly inhibited Pneumocystis carinii growth in vitro at 1 microgram/ml. This activity was similar to that of primaquine. In rat therapy models, the WRAIR compounds affected Pneumocystis pneumonia at doses as low as 0.25 mg/kg (WR242511) or 0.5 mg/kg (WR6026 and WR238605). At these doses, primaquine alone was ineffective as therapy. In a rat prophylaxis model, all three WRAIR 8-aminoquinolines were extremely effective at daily doses of 0.57 mg/kg, showing activity greater than that of primaquine at this dosage and comparable to that of trimethoprim-sulfamethoxazole at 50/250 mg/kg.

• Authors: M S Bartlett, S F Queener, R R Tidwell, W K Milhous, J D Berman, W Y Ellis, J W Smith
• Journal: Antimicrobial agents and chemotherapy (Antimicrob Agents Chemother) Vol. 35 Issue 2 Pg. 277-82 (Feb 1991) ISSN: 0066-4804 [Print] United States
• PMID: 2024961 (Publication Type: Journal Article, Research Support, U.S. Gov't, P.H.S.)

Chemical References

• Aminoquinolines
• Clindamycin
• Trimethoprim, Sulfamethoxazole Drug Combination
• Primaquine

Topics

• Aminoquinolines (therapeutic use)
• Animals
• Clindamycin (therapeutic use)
• Drug Therapy, Combination
• Female
• Lung (microbiology)
• Male
• Pneumonia, Pneumocystis (drug therapy, microbiology, prevention & control)
• Primaquine (therapeutic use)
• Rats
• Rats, Inbred Strains
• Trimethoprim, Sulfamethoxazole Drug Combination (therapeutic use)