Anti-Pneumocystis carinii pneumonia activity of dicationic 2,4-diarylpyrimidines.
Anti-Pneumocystis carinii pneumonia activity of dicationic 2,4-diarylpyrimidines.
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双2,4-二芳基嘧啶的抗卡氏肺囊虫肺炎活性。
DOI：
10.1016/0223-5234(96)83970-5
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发表时间：
1996
影响因子：
6.7
通讯作者：
Tidwell,R
中科院分区：
文献类型：
--
作者：
Kumar,A;Boykin,D;Wilson,W;Jones,S;Bender,B;Dykstra,C;Hall,J;Tidwell,R
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-bromoaceto-phenone is reported. A synthesis of 2-(4-amidinopnenyl)-4-(2-methoxy-4-amidinophenyl)pyrimidine 20, 2-[4-(imidazolin2-yl)-phenyl]-4-[2-me thoxy-4-(imidazolin-2-yl)phenyl]pyrimidine 21, and 2-[4-(N-iso-propylamidino)phenyl]-4-[2-methoxy-4-(N-isopro-pylamidino)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.
