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利用裸鼠开展新型抗麻风化疗药物的研究,特别提及一种新型喹诺酮羧酸类药物AT - 4140。

Studies on the development of novel anti-leprous chemotherapeutics using nude mice with special reference to a new quinolone carboxylic acid, AT-4140.

作者信息

Tsutsumi S, Gidoh M

出版信息

Nihon Rai Gakkai Zasshi. 1989 Oct-Dec;58(4):250-8. doi: 10.5025/hansen1977.58.250.

DOI:10.5025/hansen1977.58.250
PMID:2489283
Abstract

In order to develop a novel drug for antileprosy chemotherapy, the inhibitory effects of three synthesized compounds, a supplied antituberculous one and three quinolone carboxylic acids were examined on the growth of leprosy bacilli inoculated into the footpads of nude mice. Amongst them, a new quinolone carboxylic acid, AT-4140 whose chemical structure was 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-7-(cis-3, 5-dimethyl-1-piperazinyl)-4-oxoquinoline-3-carboxylic acid strongly inhibited the growth of leprosy bacilli at doses of 15 and 30 mg/kg. Whereas, the effect of Ofloxacin used as a positive control was limited at the same doses.

摘要

为开发一种用于麻风病化疗的新型药物,研究了三种合成化合物、一种提供的抗结核药物以及三种喹诺酮羧酸对接种于裸鼠足垫的麻风杆菌生长的抑制作用。其中,一种化学结构为5-氨基-1-环丙基-6,8-二氟-1,4-二氢-7-(顺式-3,5-二甲基-1-哌嗪基)-4-氧代喹啉-3-羧酸的新型喹诺酮羧酸AT-4140,在15和30mg/kg剂量时能强烈抑制麻风杆菌生长。而作为阳性对照的氧氟沙星在相同剂量下作用有限。

相似文献

1
Studies on the development of novel anti-leprous chemotherapeutics using nude mice with special reference to a new quinolone carboxylic acid, AT-4140.利用裸鼠开展新型抗麻风化疗药物的研究,特别提及一种新型喹诺酮羧酸类药物AT - 4140。
Nihon Rai Gakkai Zasshi. 1989 Oct-Dec;58(4):250-8. doi: 10.5025/hansen1977.58.250.
2
Activity of sparfloxacin against Mycobacterium leprae inoculated into footpads of nude mice.司帕沙星对接种于裸鼠足垫的麻风分枝杆菌的活性。
Lepr Rev. 1992 Jun;63(2):108-16.
3
Activity of sparfloxacin against Mycobacterium leprae measured by the proportional bactericidal test.通过比例杀菌试验测定司帕沙星对麻风分枝杆菌的活性。
Int J Lepr Other Mycobact Dis. 1993 Dec;61(4):605-8.
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A Mycobacterium leprae isolate resistant to dapsone, rifampin, ofloxacin and sparfloxacin.一株对氨苯砜、利福平、氧氟沙星和司帕沙星耐药的麻风分枝杆菌分离株。
Int J Lepr Other Mycobact Dis. 2000 Dec;68(4):452-5.
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Inhibition of the multiplication of Mycobacterium leprae in nude mice by intermittent administration of a new rifamycin derivative, 3'-hydroxy-5'-(4-isobutyl-1-piperazinyl)benzoxazinorifamycin (KRM-1648) combined with sparfloxacin.通过间歇性给予一种新型利福霉素衍生物3'-羟基-5'-(4-异丁基-1-哌嗪基)苯并恶嗪并利福霉素(KRM-1648)与司帕沙星联合使用,抑制麻风分枝杆菌在裸鼠体内的繁殖。
Lepr Rev. 1995 Mar;66(1):39-47. doi: 10.5935/0305-7518.19950006.
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Anti-Mycobacterium leprae activity of several quinolones studied in the mouse.几种喹诺酮类药物在小鼠体内抗麻风分枝杆菌的活性研究。
Int J Lepr Other Mycobact Dis. 1991 Dec;59(4):613-7.
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The inhibitory effects by combined doses of DDS and several immunostimulants on the growth of leprosy bacilli inoculated into footpads of hybrid nude mice, Jcl:AF-nu.二氨二苯砜(DDS)与几种免疫刺激剂联合用药对接种于Jcl:AF-nu杂交裸鼠足垫的麻风杆菌生长的抑制作用
Nihon Rai Gakkai Zasshi. 1989 Oct-Dec;58(4):241-9. doi: 10.5025/hansen1977.58.241.
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Activities of various quinolone antibiotics against Mycobacterium leprae in infected mice.多种喹诺酮类抗生素对感染小鼠体内麻风分枝杆菌的活性。
Antimicrob Agents Chemother. 1992 Nov;36(11):2544-7. doi: 10.1128/AAC.36.11.2544.
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Bactericidal activities of single or multiple doses of various combinations of new antileprosy drugs and/or rifampin against M. leprae in mice.新型抗麻风病药物和/或利福平的单剂量或多剂量不同组合对小鼠体内麻风分枝杆菌的杀菌活性。
Int J Lepr Other Mycobact Dis. 1992 Dec;60(4):556-61.
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The chemotherapy of leprosy. Part 2.麻风病的化学疗法。第2部分。
Int J Lepr Other Mycobact Dis. 1991 Mar;59(1):82-94.

引用本文的文献

1
Clinical trial of sparfloxacin for lepromatous leprosy.司帕沙星治疗瘤型麻风的临床试验。
Antimicrob Agents Chemother. 1994 Jan;38(1):61-5. doi: 10.1128/AAC.38.1.61.
2
Chemotherapy of lepromatous leprosy: recent developments and prospects for the future.瘤型麻风的化学疗法:近期进展与未来展望
Eur J Clin Microbiol Infect Dis. 1994 Nov;13(11):942-52. doi: 10.1007/BF02111496.
3
In vitro activities of aminoglycosides, lincosamides, and rifamycins against Mycobacterium leprae.氨基糖苷类、林可酰胺类和利福霉素类药物对麻风分枝杆菌的体外活性
Antimicrob Agents Chemother. 1991 Jun;35(6):1232-4. doi: 10.1128/AAC.35.6.1232.
4
Activities of various quinolone antibiotics against Mycobacterium leprae in infected mice.多种喹诺酮类抗生素对感染小鼠体内麻风分枝杆菌的活性。
Antimicrob Agents Chemother. 1992 Nov;36(11):2544-7. doi: 10.1128/AAC.36.11.2544.