Potent antibacterial fluoroquinolones with marked activity againstLeishmania donovani in vivo

Raether, W.; Seidenath, H.; Hofmann, Johannes

doi:10.1007/bf00931138

Cited by 21 publications

(11 citation statements)

References 12 publications

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“…The crude product thus obtained was chromatographed over silica gel column. Elution of the column with CHCl 3 : MeOH: CH 3 …”

Section: -Amino-6(7h)-oxo-1-hydroxyethoxymethyl-pyrazolo[34-d]pyrimmentioning

confidence: 99%

“…[1] The biochemical targets being pursued for design of suitable chemotherapeutic agents include inhibitors of purine salvage pathways, [2] DNAgyrase, [3] tubulin binding, [4] hydroperoxide metabolism, [5] and trypanothione reductase. [6] The parasite has evolved a unique mechanism for scavenging purines and their nucleotides from the host in absence of its de-novo synthesis.…”

Section: Introductionmentioning

confidence: 99%

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Acyclic Pyrazolo[3,4- d ]Pyrimidine Nucleoside as Potential Leishmaniostatic Agent *

Hasan¹,

Satyanarayana²,

Mishra³

et al. 2006

Nucleosides, Nucleotides & Nucleic Acids

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A new synthesis of 6-amino-1-hydroxyethoxymethyl-4 (5H)-oxopyrazolo[3, 4-d]pyrimidine (4) has been mentioned. Compound 4 exhibited inhibition of amastigotes of Leishmania donovani to the extent of 89 % at 30 microg/mL, whereas iso-guanine analogue 5 had the inhibition only to the extent of 52.8% at 100 microg/mL in vitro. In hamster model the maximum inhibitory response for compound 4 against amastigotes multiplication was observed to be 94% at 50 mg/kg single dose for 5 consecutive days.

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“…The crude product thus obtained was chromatographed over silica gel column. Elution of the column with CHCl 3 : MeOH: CH 3 …”

Section: -Amino-6(7h)-oxo-1-hydroxyethoxymethyl-pyrazolo[34-d]pyrimmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Acyclic Pyrazolo[3,4- d ]Pyrimidine Nucleoside as Potential Leishmaniostatic Agent *

Hasan¹,

Satyanarayana²,

Mishra³

et al. 2006

Nucleosides, Nucleotides & Nucleic Acids

View full text Add to dashboard Cite

show abstract

“…Another reason for the strong interest in this subject is that the genomic structure of trypanosomes exhibits major similarities with bacteria, so that fluoroquinolones could potentially also interfere with DNA replication in some protozoans from the class Trypanosomidae, such as L. infantum (Chakraborty and Majumder 1988;Slunt et al 1996). Some evidence exists of the possible activity of fluoroquinolones, tested both in vitro and in vivo against such pathogens (Raether et al 1989;Furet and Peche`re 1991;Werbovetz et al 1992;Croft and Hogg 1998). Another particularly important characteristic of enrofloxacin is its remarkable capacity to penetrate the intracellular environment and to be carried via active transport by macrophages and neutrophils, helping concomitantly both phagocytosis and the killing activity of these cells (Boeckh et al 1999).…”

Section: Introductionmentioning

confidence: 95%

The efficacy of enrofloxacin, alone or combined with metronidazole, in the therapy of canine leishmaniasis

et al. 2004

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We evaluated the efficacy of enrofloxacin, alone or combined with metronidazole, against Leishmania infantum. The in vitro activity of this fluoroquinolone was assessed using two different methods: a direct test aimed at assessing the drug activity on the parasite, and an indirect test aimed at evaluating the drug effect on macrophage killing, lymphomonocyte activation and nitric oxide production. An in vivo test was also performed on 36 dogs with leishmaniasis, subdivided into three groups, one treated with enrofloxacin, another with enrofloxacin plus metronidazole, and a control group with meglumine antimoniate. The direct test did not show any action of enrofloxacin on the parasite, while the indirect testing showed an enhancement of macrophage killing and an increase in nitric oxide production. These findings show that enrofloxacin does not exert a direct anti-leishmanial activity in vitro. However, on the basis of the positive immunostimulation results shown in vitro and the clinical improvement, particularly of the cutaneous lesions, obtained in several dogs in the in vivo trial, the use of enrofloxacin in association with a specific anti-leishmanial drug can be proposed in the therapeutic protocol of canine leishmaniasis.

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“…Recently miltefosine has been registered for use in dogs and different studies have demonstrated its leishmanicidal effect (Mirò et al 2009). Moreover, it has been suggested that fluoroquinolones, compared to standard chemotherapeutic agents, coul d be an effective and pragmatic alternative to treat CVL (Raether et al 1989;Vouldoukis et al 2006). …”

Section: Introductionmentioning

confidence: 98%

Canine leishmaniosis: in vitro efficacy of miltefosine and marbofloxacin alone or in combination with allopurinol against clinical strains of Leishmania infantum

et al. 2012

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Despite the availability of different therapeutic options, canine visceral leishmaniosis (CVL) remains a challenging disease to treat. Recently miltefosine has been registered for use in dogs, and different studies have demonstrated its leishmanicidal effect. Moreover, it has been suggested that fluoroquinolones, compared to standard chemotherapeutic agents, could be an effective and pragmatic alternative to treat CVL. The efficacy of miltefosine and marbofloxacin alone or in combination with allopurinol against clinical strains of Leishmania infantum was assessed in vitro by incubating increasing concentrations of the drugs with a standard parasite inoculum. Miltefosine was significantly more efficacious than marbofloxacin (P < 0.05) against the two strains of L. infantum either alone or in combination with allopurinol. Both drugs were significantly (P < 0.05) more efficacious when associated with allopurinol than alone.

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Potent antibacterial fluoroquinolones with marked activity againstLeishmania donovani in vivo

Cited by 21 publications

References 12 publications

Acyclic Pyrazolo[3,4- d ]Pyrimidine Nucleoside as Potential Leishmaniostatic Agent *

Acyclic Pyrazolo[3,4- d ]Pyrimidine Nucleoside as Potential Leishmaniostatic Agent *

The efficacy of enrofloxacin, alone or combined with metronidazole, in the therapy of canine leishmaniasis

Canine leishmaniosis: in vitro efficacy of miltefosine and marbofloxacin alone or in combination with allopurinol against clinical strains of Leishmania infantum

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