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Literature DB >> 2334166

Influence of N substitution on antimycobacterial activity of ciprofloxacin.

A Haemers¹, D C Leysen, W Bollaert, M Q Zhang, S R Pattyn.

Abstract

Ciprofloxacin analogs with various substitutions on the piperazine nitrogen were tested against several mycobacteria. In contrast to what has been found with other gram-positive and gram-negative bacteria, alkyl analogs such as N-isopropylciprofloxacin were shown to be significantly more active than ciprofloxacin. MICs of 0.125 microgram/ml against Mycobacterium tuberculosis were found.

Entities: Chemical Species

Mesh：

Substances：
Ciprofloxacin

Year: 1990 PMID： 2334166 PMCID： PMC171627 DOI： 10.1128/AAC.34.3.496

Source DB: PubMed Journal: Antimicrob Agents Chemother ISSN： 0066-4804 Impact factor: 5.191

3 in total

Review 1. Structure-activity relationships of the fluoroquinolones.

Authors: D T Chu; P B Fernandes
Journal: Antimicrob Agents Chemother Date: 1989-02 Impact factor: 5.191

Review 2. Mycobacteria and the new quinolones.

Authors: D C Leysen; A Haemers; S R Pattyn
Journal: Antimicrob Agents Chemother Date: 1989-01 Impact factor: 5.191

3. Structure-activity relationships of antibacterial 6,7- and 7,8-disubstituted 1-alkyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acids.

Authors: H Koga; A Itoh; S Murayama; S Suzue; T Irikura
Journal: J Med Chem Date: 1980-12 Impact factor: 7.446

3 in total

9 in total

Review 1. Penetration of lipophilic agents with multiple protonation sites into bacterial cells: tetracyclines and fluoroquinolones as examples.

Authors: H Nikaido; D G Thanassi
Journal: Antimicrob Agents Chemother Date: 1993-07 Impact factor: 5.191

Influence of N substitution on antimycobacterial activity of ciprofloxacin.

Review 1. Structure-activity relationships of the fluoroquinolones.

Review 2. Mycobacteria and the new quinolones.

3. Structure-activity relationships of antibacterial 6,7- and 7,8-disubstituted 1-alkyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acids.

Review 1. Penetration of lipophilic agents with multiple protonation sites into bacterial cells: tetracyclines and fluoroquinolones as examples.

2. Antimycobacterial activities of novel levofloxacin analogues.

Review 3. Newly documented antimicrobial activity of quinolones.

4. In vitro susceptibilities of rapidly growing mycobacteria to newer antimicrobial agents.

5. Role of porins for uptake of antibiotics by Mycobacterium smegmatis.

6. Design, synthesis and antimycobacterial activities of 1-methyl-2-alkenyl-4(1H)-quinolones.

7. Facile synthesis and antimycobacterial activity of isoniazid, pyrazinamide and ciprofloxacin derivatives.

Review 8. Drug Resistance in Nontuberculous Mycobacteria: Mechanisms and Models.

9. Polyamines inhibit porin-mediated fluoroquinolone uptake in mycobacteria.