阳离子取代双苯并咪唑对实验性卡氏肺孢子虫肺炎的活性。
Activity of cationically substituted bis-benzimidazoles against experimental Pneumocystis carinii pneumonia.
作者信息
Tidwell R R, Jones S K, Naiman N A, Berger L C, Brake W B, Dykstra C C, Hall J E
机构信息
Department of Pathology, School of Medicine, University of North Carolina, Chapel Hill 27599.
出版信息
Antimicrob Agents Chemother. 1993 Aug;37(8):1713-6. doi: 10.1128/AAC.37.8.1713.
Abstract
On the basis of a previously observed correlation between the antimicrobial activity and DNA binding strength of dicationic molecules, a series of 10 dicationically substituted bis-benzimidazoles were tested for activity in the rat model of Pneumocystis carinii pneumonia. One of the compounds, 1,4-bis[5-(2-imidazolinyl)-2-benzimidazolyl]butane, was found to be more potent and less toxic than pentamidine.
摘要
基于先前观察到的双阳离子分子的抗菌活性与DNA结合强度之间的相关性，对一系列10种双阳离子取代的双苯并咪唑进行了卡氏肺孢子虫肺炎大鼠模型中的活性测试。其中一种化合物，1,4 - 双[5 - (2 - 咪唑啉基)-2 - 苯并咪唑基]丁烷，被发现比喷他脒更有效且毒性更小。
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本文引用的文献
1
[A new method of treating interstitial plasma cell pneumonia in premature infant with 5-valent antimony & aromatic diamidines].[用五价锑与芳香二脒治疗早产儿间质性浆细胞肺炎的新方法]
Monatsschr Kinderheilkd (1902). 1958 Jan;106(1):10-4.
2
Present status of chemotherapy and chemopropylaxis of human trypanosomiasis in the Eastern Hemisphere.
Pharmacol Ther. 1980;11(2):391-413. doi: 10.1016/0163-7258(80)90035-2.
3
Efficacy of trimethoprim and sulfamethoxazole in the prevention and treatment of Pneumocystis carinii pneumonitis.甲氧苄啶和磺胺甲恶唑在预防和治疗卡氏肺孢子虫肺炎中的疗效。
Antimicrob Agents Chemother. 1974 Mar;5(3):289-93. doi: 10.1128/AAC.5.3.289.
4
A rapid staining procedure for Pneumocystis carinii.卡氏肺孢子虫的快速染色程序。
Am J Med Technol. 1973 Jul;39(7):267-8.
5
Cationic antitrypanosomal and other antimicrobial agents in the therapy of experimental Pneumocystis carinii pneumonia.阳离子抗锥虫药及其他抗菌药物在实验性卡氏肺孢子虫肺炎治疗中的应用
Antimicrob Agents Chemother. 1988 Jun;32(6):896-905. doi: 10.1128/AAC.32.6.896.
6
Visceral leishmaniasis unresponsive to antimonial drugs. II. Response to high dosage sodium stibogluconate or prolonged treatment with pentamidine.对锑剂无反应的内脏利什曼病。II. 对高剂量葡糖酸锑钠或喷他脒延长治疗的反应
Trans R Soc Trop Med Hyg. 1985;79(5):705-14. doi: 10.1016/0035-9203(85)90199-3.
7
Prevention of Pneumocystis carinii pneumonia by inhaled pentamidine.吸入喷他脒预防卡氏肺孢子虫肺炎
Lancet. 1989 Mar 25;1(8639):654-7. doi: 10.1016/s0140-6736(89)92153-3.
8
Novel pentamidine analogs in the treatment of experimental Pneumocystis carinii pneumonia.新型喷他脒类似物治疗实验性卡氏肺孢子虫肺炎
Antimicrob Agents Chemother. 1990 Jun;34(6):1026-30. doi: 10.1128/AAC.34.6.1026.
9
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J Med Chem. 1990 Apr;33(4):1252-7. doi: 10.1021/jm00166a026.
10
Structure-activity relationships of analogs of pentamidine against Plasmodium falciparum and Leishmania mexicana amazonensis.喷他脒类似物对恶性疟原虫和亚马逊利什曼原虫的构效关系
Antimicrob Agents Chemother. 1990 Jul;34(7):1381-6. doi: 10.1128/AAC.34.7.1381.
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