• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

相似文献

1
Activity of lipid-soluble inhibitors of dihydrofolate reductase against Pneumocystis carinii in culture and in a rat model of infection.二氢叶酸还原酶的脂溶性抑制剂在体外培养及大鼠感染模型中对卡氏肺孢子虫的活性
Antimicrob Agents Chemother. 1987 Sep;31(9):1323-7. doi: 10.1128/AAC.31.9.1323.
2
Efficacy of trimetrexate, a potent lipid-soluble antifolate, in the treatment of rodent Pneumocystis carinii pneumonia.三甲曲沙（一种强效脂溶性抗叶酸剂）治疗啮齿动物卡氏肺孢子虫肺炎的疗效。
Am J Trop Med Hyg. 1988 Nov;39(5):491-6. doi: 10.4269/ajtmh.1988.39.491.
3
Lipophilic antifolates as agents against opportunistic infections. 1. Agents superior to trimetrexate and piritrexim against Toxoplasma gondii and Pneumocystis carinii in in vitro evaluations.亲脂性抗叶酸剂作为抗机会性感染的药物。1. 在体外评估中对弓形虫和卡氏肺孢子虫优于三甲曲沙和吡利曲辛的药物。
J Med Chem. 1996 Mar 15;39(6):1271-80. doi: 10.1021/jm950760y.
4
Potent antipneumocystis and antitoxoplasma activities of piritrexim, a lipid-soluble antifolate.脂溶性抗叶酸剂吡利昔明具有强大的抗肺孢子菌和抗弓形虫活性。
Antimicrob Agents Chemother. 1988 Apr;32(4):430-3. doi: 10.1128/AAC.32.4.430.
5
Evaluation of potent inhibitors of dihydrofolate reductase in a culture model for growth of Pneumocystis carinii.在卡氏肺孢子虫生长的培养模型中对二氢叶酸还原酶强效抑制剂的评估。
Antimicrob Agents Chemother. 1995 Nov;39(11):2436-41. doi: 10.1128/AAC.39.11.2436.
6
2,4-Diaminothieno[2,3-d]pyrimidine analogues of trimetrexate and piritrexim as potential inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase.三甲曲沙和吡利曲辛的2,4-二氨基噻吩并[2,3-d]嘧啶类似物作为卡氏肺孢子虫和刚地弓形虫二氢叶酸还原酶的潜在抑制剂。
J Med Chem. 1993 Oct 15;36(21):3103-12. doi: 10.1021/jm00073a009.
7
Tricyclic 2,4-diaminopyrimidines with broad antifolate activity and the ability to inhibit Pneumocystis carinii growth in cultured human lung fibroblasts in the presence of leucovorin.具有广泛抗叶酸活性且在亚叶酸存在下能够抑制人肺成纤维细胞培养物中卡氏肺孢子虫生长的三环2,4 - 二氨基嘧啶。
Biochem Pharmacol. 1989 Aug 15;38(16):2677-84. doi: 10.1016/0006-2952(89)90554-6.
8
Pneumocystis carinii dihydrofolate reductase used to screen potential antipneumocystis drugs.卡氏肺孢子虫二氢叶酸还原酶用于筛选潜在的抗肺孢子虫药物。
Antimicrob Agents Chemother. 1991 Jul;35(7):1348-55. doi: 10.1128/AAC.35.7.1348.
9
Trimetrexate for the treatment of Pneumocystis carinii pneumonia in patients with the acquired immunodeficiency syndrome.三甲曲沙用于治疗获得性免疫缺陷综合征患者的卡氏肺孢子虫肺炎。
N Engl J Med. 1987 Oct 15;317(16):978-85. doi: 10.1056/NEJM198710153171602.
10
Inhibition of Pneumocystis dihydrofolate reductase by analogs of pyrimethamine, methotrexate and trimetrexate.乙胺嘧啶、甲氨蝶呤和三甲曲沙类似物对肺孢子菌二氢叶酸还原酶的抑制作用。
J Protozool. 1991 Nov-Dec;38(6):154S-157S.

引用本文的文献

1
Opportunistic infections in HIV-infected patients.HIV感染患者的机会性感染。
Can J Infect Dis. 1992 Mar;3(2):82-7. doi: 10.1155/1992/413713.
2
Towards new antifolates targeting eukaryotic opportunistic infections.靶向真核生物机会性感染的新型抗叶酸剂研究进展
Eukaryot Cell. 2009 Apr;8(4):483-6. doi: 10.1128/EC.00298-08. Epub 2009 Jan 23.
3
A genetic algorithm for structure-based de novo design.一种基于结构的从头设计的遗传算法。
J Comput Aided Mol Des. 2001 Oct;15(10):911-33. doi: 10.1023/a:1014389729000.
4
Dicyclic and tricyclic diaminopyrimidine derivatives as potent inhibitors of Cryptosporidium parvum dihydrofolate reductase: structure-activity and structure-selectivity correlations.双环和三环二氨基嘧啶衍生物作为微小隐孢子虫二氢叶酸还原酶的有效抑制剂：构效关系和构选关系
Antimicrob Agents Chemother. 2001 Dec;45(12):3293-303. doi: 10.1128/AAC.45.12.3293-3303.2001.
5
Expression and characterization of recombinant human-derived Pneumocystis carinii dihydrofolate reductase.重组人源卡氏肺孢子虫二氢叶酸还原酶的表达与鉴定
Antimicrob Agents Chemother. 2000 Nov;44(11):3092-6. doi: 10.1128/AAC.44.11.3092-3096.2000.
6
In vitro and in vivo immunomodulatory effects of anti-Pneumocystis carinii drugs.抗卡氏肺孢子虫药物的体外和体内免疫调节作用。
Antimicrob Agents Chemother. 1996 May;40(5):1294-7. doi: 10.1128/AAC.40.5.1294.
7
Activity of topoisomerase inhibitors against Pneumocystis carinii in vitro and in an inoculated mouse model.拓扑异构酶抑制剂对卡氏肺孢子虫的体外活性及在接种小鼠模型中的活性。
Antimicrob Agents Chemother. 1993 Jul;37(7):1543-6. doi: 10.1128/AAC.37.7.1543.
8
Total cellular fatty acid composition of cultured Pneumocystis carinii.培养的卡氏肺孢子虫的全细胞脂肪酸组成
J Clin Microbiol. 1993 Jul;31(7):1899-902. doi: 10.1128/jcm.31.7.1899-1902.1993.
9
Close association of Pneumocystis carinii from infected rat lung with culture cells as shown by light and electron microscopy.通过光学显微镜和电子显微镜观察发现，感染大鼠肺中的卡氏肺孢子虫与培养细胞紧密相连。
Parasitol Res. 1994;80(3):208-15. doi: 10.1007/BF00932676.
10
Trimetrexate. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential in the treatment of Pneumocystis carinii pneumonia.三甲曲沙。对其药效学和药代动力学特性以及在治疗卡氏肺孢子虫肺炎中的治疗潜力的综述。
Drugs. 1995 Apr;49(4):563-76. doi: 10.2165/00003495-199549040-00007.

本文引用的文献

1
Synthesis and antitumor activity of 2,4-diamino-6-(2,5-dimethoxybenzyl)-5-methylpyrido[2,3-d]pyrimidine.2,4-二氨基-6-(2,5-二甲氧基苄基)-5-甲基吡啶并[2,3-d]嘧啶的合成及其抗肿瘤活性
J Med Chem. 1980 Mar;23(3):327-9. doi: 10.1021/jm00177a025.
2
Inhibition of histamine-metabolizing enzymes and elevation of histamine levels in tissues by lipid-soluble anticancer folate antagonists.
Mol Pharmacol. 1980 Jul;18(1):100-4.
3
Growth and serial passage of Pneumocystis carinii in the A549 cell line.卡氏肺孢子虫在A549细胞系中的生长及连续传代
Infect Immun. 1984 May;44(2):245-51. doi: 10.1128/iai.44.2.245-251.1984.
4
Pharmacology and toxicity of a potent "nonclassical" 2,4-diamino quinazoline folate antagonist, trimetrexate, in normal dogs.强效“非经典”2,4-二氨基喹唑啉叶酸拮抗剂三甲曲沙在正常犬体内的药理学与毒性研究
Cancer Res. 1982 May;42(5):1696-702.
5
Successful treatment of lethal protozoal infections with the ornithine decarboxylase inhibitor, alpha-difluoromethylornithine.用鸟氨酸脱羧酶抑制剂α-二氟甲基鸟氨酸成功治疗致死性原生动物感染。
Trans Assoc Am Physicians. 1984;97:70-9.
6
Adverse reactions to trimethoprim-sulfamethoxazole in patients with the acquired immunodeficiency syndrome.获得性免疫缺陷综合征患者对甲氧苄啶-磺胺甲恶唑的不良反应。
Ann Intern Med. 1984 Apr;100(4):495-9. doi: 10.7326/0003-4819-100-4-495.
7
Complications of co-trimoxazole in treatment of AIDS-associated Pneumocystis carinii pneumonia in homosexual men.复方新诺明治疗同性恋男性艾滋病相关卡氏肺孢子虫肺炎的并发症
Lancet. 1983 Nov 12;2(8359):1109-11. doi: 10.1016/s0140-6736(83)90627-x.
8
Latent Pneumocystis infection of rats, relapse, and chemotherapy.大鼠的潜伏性肺孢子菌感染、复发及化疗
Lab Invest. 1966 Oct;15(10):1559-77.
9
Pentamidine for the treatment of Pneumocystis carinii pneumonia and other protozoal diseases.喷他脒用于治疗卡氏肺孢子虫肺炎及其他原生动物疾病。
Ann Intern Med. 1985 Nov;103(5):782-6. doi: 10.7326/0003-4819-103-5-782.
10
Antimicrobial susceptibility of Pneumocystis carinii in culture.卡氏肺孢子菌在培养中的药敏性。
Diagn Microbiol Infect Dis. 1985 Sep;3(5):381-7. doi: 10.1016/0732-8893(85)90076-8.

二氢叶酸还原酶的脂溶性抑制剂在体外培养及大鼠感染模型中对卡氏肺孢子虫的活性

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

作者信息

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

机构信息

Department of Pharmacology, Indiana University School of Medicine, Indianapolis 46223.

出版信息

Antimicrob Agents Chemother. 1987 Sep;31(9):1323-7. doi: 10.1128/AAC.31.9.1323.

DOI:10.1128/AAC.31.9.1323
PMID:2445281
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC174935/
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 microgram of trimetrexate or BW301U per ml. Trimethoprim is ineffective at 100 micrograms/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.

摘要

三甲曲沙和BW301U（吡曲克辛羟乙磺酸盐）是二氢叶酸还原酶的脂溶性抑制剂，在与WI-38细胞共培养时，它们是卡氏肺孢子虫生长的强效抑制剂。每毫升含0.1微克三甲曲沙或BW301U时即可观察到抑制作用。在该培养系统中，甲氧苄啶在100微克/毫升时无效。三甲曲沙和BW301U作为大鼠卡氏肺孢子虫肺炎的预防药物均有效；7.5毫克/千克的三甲曲沙保护了10只大鼠中的9只，5毫克/千克的BW301U保护了10只大鼠中的4只。