160523-01-3Relevant academic research and scientific papers
Anti-Pneumocystis carinii pneumonia activity of dicationic 2,4-diarylpyrimidines
Kumar,Boykin,Wilson,Jones,Bender,Dykstra,Hall,Tidwell
, p. 767 - 773 (2007/10/03)
A synthesis of 2,4-bis-(4-amidinophenyl)pyrimidine 6, 2,4-bis-[(4-imidazolin-2-yl)phenyl)]pyrimidine 7, 2,4-bis[(4-tetrahydropyrimidinyl-2-yl)phenyl]pyrimidine 8, 2,4-bis[(4-N-n-propylamidino)phenyl]pyrimidine 9, 2,4-bis[(4-N-isopropylamidino)phenyl]pyrimidine 10 and 2,4-bis[(4-N-isobutylamidino)phenyl]pyrimidine 11 starting from 4-bromobenzamidine and 4-bromoacetophenone is reported. A synthesis of 2-(4-amidinophenyl)-4-(2-methoxy-4-amidinophenyl)pyrimidine 20, 2-[4-(imidazolin-2-yl)- phenyl]-4-[2-methoxy-4-(imidazolin-2-yl)phenyl]pyrimidine 21, and 2-[4-(N-iso-propylamidino)phenyl]-4-[2-methoxy-4-(N -isopropylamidino)phenyl]pyrimidine 22 beginning with 4-bromobenzamidine and 2-methoxy-4-bromoacetophenone is described. Compounds 6-11 and 20-22 all bind strongly to DNA. Compounds 6, 9-11, and 20 given at 5 mg/kg are more active and less toxic than pentamidine at its effective dose when evaluated against Pneumocystis carinii pneumonia (PCP) in the immunosuppressed rat model. Several compounds in this series are being evaluated further as potential new anti-PCP agents.
Methods of treating pneumocystis carinii pneumonia
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, (2008/06/13)
The present invention provides methods for treating Pneumocystis carinii pneumonia and Giardia lamblia in a subject in need of such treatment. The methods comprises administering to the subject a compound of Formula I: STR1 wherein: X and Y are located in
