吡哌酸，一种对铜绿假单胞菌有效的新型抗菌剂：体外特性

Pipemidic acid, a new antibacterial agent active against Pseudomonas aeruginosa: in vitro properties.

作者信息

Shimizu M, Takase Y, Nakamura S, Katae H, Minami A

出版信息

Antimicrob Agents Chemother. 1975 Aug;8(2):132-8. doi: 10.1128/AAC.8.2.132.

DOI:10.1128/AAC.8.2.132

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC429279/

Abstract

Pipemidic acid, 8-ethyl-5,8-dihydro-5-oxo-2-(1-piperazinyl)-pyrido [2,3-d]pyrimidine-6-carboxylic acid, is a new derivative of piromidic acid. It is active against gram-negative bacteria including Pseudomonas aeruginosa as well as some gram-positive bacteria. Its potency is generally greater than that of piromidic acid and nalidixic acid. Cross-resistance is not observed between pipemidic acid and various antibiotics, and most of bacteria resistant to piromidic acid and nalidixic acid are moderately susceptible to pipemidic acid. The activity of pipemidic acid is scarcely affected by the addition of serum, sodium cholate, or change of medium pH, but is subject to the influence of inoculum size. Its action is bactericidal above minimal inhibitory concentrations.

摘要

吡哌酸，8-乙基-5,8-二氢-5-氧代-2-(1-哌嗪基)吡啶并[2,3-d]嘧啶-6-羧酸，是吡咯米酸的一种新衍生物。它对包括铜绿假单胞菌在内的革兰氏阴性菌以及一些革兰氏阳性菌具有活性。其效力通常大于吡咯米酸和萘啶酸。在吡哌酸与各种抗生素之间未观察到交叉耐药性，并且大多数对吡咯米酸和萘啶酸耐药的细菌对吡哌酸中度敏感。吡哌酸的活性几乎不受血清、胆酸钠添加或培养基pH值变化的影响，但受接种量大小的影响。在最低抑菌浓度以上其作用是杀菌性的。

相似文献

1

Pipemidic acid, a new antibacterial agent active against Pseudomonas aeruginosa: in vitro properties.

Antimicrob Agents Chemother. 1975 Aug;8(2):132-8. doi: 10.1128/AAC.8.2.132.

2

In vitro antibacterial activity of AM-715, a new nalidixic acid analog.

Antimicrob Agents Chemother. 1980 Feb;17(2):103-8. doi: 10.1128/AAC.17.2.103.

3

In vitro antibacterial properties of AT-2266, a new pyridonecarboxylic acid.

Antimicrob Agents Chemother. 1983 May;23(5):641-8. doi: 10.1128/AAC.23.5.641.

4

Researches on antibacterial and antifungal agents. II - Synthesis of 1-ethyl-1,4-dihydro-4-oxo-7-(1-pyrrolidinyl)quinoline-3-carboxylic acid, a novel highly active, broad-spectrum antibacterial agent related to piromidic acid.

Farmaco Sci. 1984 Feb;39(2):95-109.

5

In vitro and in vivo antibacterial activity of AT-2266.

Antimicrob Agents Chemother. 1983 Jul;24(1):78-84. doi: 10.1128/AAC.24.1.78.

6

[Antibacterial in-vitro activity of pipemidic acid and nalidixic acid (author's transl)].

Dtsch Med Wochenschr. 1979 Jun 29;104(26):946-8. doi: 10.1055/s-0028-1104021.

7

In vitro and in vivo activity of DL-8280, a new oxazine derivative.

Antimicrob Agents Chemother. 1982 Oct;22(4):548-53. doi: 10.1128/AAC.22.4.548.

8

Pyrido(2,3-d)pyrimidine antibacterial agents. 3. 8-Alkyl- and 8-vinyl-5,8-dihydro-5-oxo-2-(1-piperazinyl)pyrido(2,3-d)pyrimidine-6-carboxylic acids and their derivatives.

J Med Chem. 1975 Jan;18(1):74-9. doi: 10.1021/jm00235a017.

9

Research on antibacterial and antifungal agents. III. Synthesis of 1-ethyl-1,4-dihydro-4-oxo-7-(1-pyrryl)quinoline-3-carboxylic acid and of some 6-derivatives.

Farmaco Sci. 1984 Nov;39(11):910-24.

10

Inhibition of conjugal transfer of R plasmids by pipemidic acid and related compounds.

Antimicrob Agents Chemother. 1976 Nov;10(5):779-85. doi: 10.1128/AAC.10.5.779.

引用本文的文献

1

Taxonomy, phylogeny, and bioactive potential of Xylariales (Sordariomycetes, Ascomycota) from Thailand: novel species discovery, new host and geographical records, and antibacterial properties.

MycoKeys. 2025 Jul 29;120:35-117. doi: 10.3897/mycokeys.120.155915. eCollection 2025.

2

Recent Development of Fluoroquinolone Derivatives as Anticancer Agents.

Molecules. 2024 Jul 27;29(15):3538. doi: 10.3390/molecules29153538.

3

Augmentation of photophysical features and Judd-Ofelt analysis of extensively green glowing terbium (III) complexes with nitrogen donor ancillary ligands.

Photochem Photobiol Sci. 2022 Nov;21(11):2011-2034. doi: 10.1007/s43630-022-00275-3. Epub 2022 Aug 6.

4

Naturally Inspired Pyrimidines Analogues for Alzheimer's Disease.

Curr Neuropharmacol. 2021;19(2):136-151. doi: 10.2174/1570159X18666201111110136.

5

A New Approach for Improving the Antibacterial and Tumor Cytotoxic Activities of Pipemidic Acid by Including It in Trimethyl-β-cyclodextrin.

Int J Mol Sci. 2019 Jan 18;20(2):416. doi: 10.3390/ijms20020416.

6

Isocratic Resolution of Fluoroquinolone-Based Antibiotics on the Phenylethyl-Bonded Phase under Nonaqueous Elution: A Consideration of the Separation Mechanism.

Int J Anal Chem. 2018 May 31;2018:1375215. doi: 10.1155/2018/1375215. eCollection 2018.

7

Nanoparticles with high payloads of pipemidic acid, a poorly soluble crystalline drug: drug-initiated polymerization and self-assembly approach.

Acta Pharm Sin B. 2018 May;8(3):420-431. doi: 10.1016/j.apsb.2018.03.008. Epub 2018 Mar 27.

8

Synthesis and in vitro antimicrobial activity screening of new pipemidic acid derivatives.

Arch Pharm Res. 2018 Jun;41(6):633-645. doi: 10.1007/s12272-018-1025-3. Epub 2018 Apr 4.

9

β-Cyclodextrin inclusion complex to improve physicochemical properties of pipemidic acid: characterization and bioactivity evaluation.

Int J Mol Sci. 2013 Jun 25;14(7):13022-41. doi: 10.3390/ijms140713022.

10

High-throughput screens for small-molecule inhibitors of Pseudomonas aeruginosa biofilm development.

Antimicrob Agents Chemother. 2007 Oct;51(10):3582-90. doi: 10.1128/AAC.00506-07. Epub 2007 Jul 30.

本文引用的文献

1

1,8-NAPHTHYRIDINE DERIVATIVES. A NEW CLASS OF CHEMOTHERAPEUTIC AGENTS.

J Med Pharm Chem. 1962 Sep;5:1063-5. doi: 10.1021/jm01240a021.

2

Pipemidic acid: absorption, distribution, and excretion.

Antimicrob Agents Chemother. 1975 Apr;7(4):441-6. doi: 10.1128/AAC.7.4.441.

3

Pyrido(2,3-d)pyrimidine antibacterial agents. 3. 8-Alkyl- and 8-vinyl-5,8-dihydro-5-oxo-2-(1-piperazinyl)pyrido(2,3-d)pyrimidine-6-carboxylic acids and their derivatives.

J Med Chem. 1975 Jan;18(1):74-9. doi: 10.1021/jm00235a017.

文献AI研究员

20分钟写一篇综述，助力文献阅读效率提升50倍。

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

文档翻译

学术文献翻译模型，支持多种主流文档格式。