Development of antibacterial agents of the nalidixic acid type

Albrecht, R.

doi:10.1007/978-3-0348-7098-6_1

Cited by 47 publications

(56 citation statements)

References 91 publications

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“…A comprehensive review of the structure-activity relationships, microbiology, and synthetic chemistry associated with the nalidixic acid-type antibacterial agents was published in 1977 (3). Since then, more than 5,000 new analogs have been described in the literature.…”

Section: Introductionmentioning

confidence: 99%

Structure-activity relationships of the fluoroquinolones

Chu

Fernandes

1989

Antimicrob Agents Chemother

274

146

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Section: Introductionmentioning

confidence: 99%

Structure-activity relationships of the fluoroquinolones

Chu

Fernandes

1989

Antimicrob Agents Chemother

274

146

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“…Since nalidixic acid (5) was found to have potent activity against gram-negative bacteria, many compounds having a 1,4-dihydro-4-oxopyridine-3-carboxylic acid moiety, which is essential for antibacterial activity, have been synthesized (2). Recently, new 4-quinolones with excellent antibacterial activities against not only gram-negative but also grampositive organisms have been developed.…”

mentioning

confidence: 99%

Synthesis and antibacterial activities of optically active ofloxacin

Hayakawa¹,

Atarashi²,

Yokohama³

et al. 1986

Antimicrob Agents Chemother

253

122

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Two optically active (100% enantiomeric excess) isomers of ofloxacin [(+/-)-ofloxacin; DL-8280; (+/-)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7 H-pyrido[1,2,3-de] [1,4] benzoxazine-6-carboxylic acid] were prepared by use of their optically resolved synthetic intermediates. One of the isomers, (-)-ofloxacin, was 8 to 128 times more potent in inhibiting the multiplication of gram-positive and gram-negative bacteria than the other, (+)-ofloxacin, and approximately two times more active than the racemate, (+/-)-ofloxacin.

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“…They could not find any abnormalities in urine output except the increased in potassium level after 100 mg/kg. The alteration after the elimination of an electrolyte using the maximum dose is not relevant with its application in practice (Albrecht, 1977). Oral doses of enrofloxacin up to 100 mg/kg (20 times the recommended dosage) showed no significant adverse effects on blood composition, blood coagulation or dieresis.…”

Section: Pharmacological Safetymentioning

confidence: 99%

“…There were no allergic or pseudoallergic effects observed conducting some in vitro test using the peritoneal mast cells. Also, the smooth muscle of the airways in guinea pigs was not affected (Albrecht, 1977). Some trials on dogs revealed that vomiting was induced only in doses far exceeding the therapeutic recommendations (>1000 mg/kg body weight (BW) PO) (Altreuther, 1987).…”

Section: Pharmacological Safetymentioning

confidence: 99%

Toxicology of baytril (enrofloxacin)

Babaahmady¹,

Khosravi²

2011

Afr. J. Pharm. Pharmacol.

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The prophylactic use of drugs, chemicals and biological substances are necessary to meet the sanitation standards used to maintain high levels of health status. The aim of this article was to present the basic data of the active substance of enrofloxacin, the pharmacokinetics, pharmacodynamics and also the pharmacological safety of this drug. Enrofloxacin as a molecule belongs to the quinolone antimicrobial family, and it is a wide spectrum antibiotic that inhibits DNA gyrase activity in bacterial cells with bactericidal effect. It is at the center of growing attention because of its potential efficacy for the treatment of diseases. This drug is a fluorinated quinolone carboxylic acid derivative, traded as baytril, which has been widely used in veterinary medicine because of its broad spectrum activity. Enrofloxacin has extensively been tested for its safety and it was proven that this medication is rarely toxic in both intravenous and oral routes. Significant side effects occurred only in laboratory animals having a 10 times higher than the recommended dose. The active substance is not teratogenic or mutagenic and in most scientific findings, there is no evidence of a potential risk to applicators and consumers. As a conclusion, it can be used in different administration routes in farm animals against a wide range of microorganism. Also, enrofloxacin is not safe to be use in poultry as Campylobacter infections have increased significantly since the use of enrofloxacin in poultry because of the resistance of such organism to fluoroquinolone groups.

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Development of antibacterial agents of the nalidixic acid type

Cited by 47 publications

References 91 publications

Structure-activity relationships of the fluoroquinolones

Structure-activity relationships of the fluoroquinolones

Synthesis and antibacterial activities of optically active ofloxacin

Toxicology of baytril (enrofloxacin)

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