4-[3,5-Bis(2-hydroxyphenyl)-1,2,4-triazol-1-yl]- benzoic Acid: A Novel Efficient and Selective Iron(III) Complexing Agent

Heinz, Uwe; Hegetschweiler, Kaspar; Acklin, Pierre; Faller, Bernard; Lattmann, René; Schnebli, Hans Peter

doi:10.1002/(sici)1521-3773(19990903)38:17<2568::aid-anie2568>3.0.co;2-c

Cited by 109 publications

(72 citation statements)

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“…In this procedure, chelator is added to the blood through a vein or administered orally in order to remove toxic element. Deferasirox (4-[3,5-bis(2-hydroxyphenyl)-1,2,4-triazol-1-yl]-benzoic acid, or ICL670; Figure 1) was first reported in 1999 (Heinz et al, 1999). It is a tridentate chelator with high selectivity for Fe 3þ , and its NO 2 donation arises from one triazole nitrogen and two phenolate oxygen donors.…”

Section: Introductionmentioning

confidence: 99%

Chelation of cadmium by combining deferasirox and deferiprone in rats

et al. 2011

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The present research aimed to characterize the potential efficiency of two chelators after cadmium administration for 60 days following two dose levels of 20 and 40 mg/kg body weight daily to male rats. However, the hypothesis that the two chelators might be more efficient as combined therapy than as single therapy in removing cadmium from the body was considered. In this way, two known chelators deferasirox and deferiprone (L(1)) were chosen and tested in the acute rat model. Two chelators were given orally as a single or combined therapy for the period of a week. Cadmium and iron concentrations in various tissues were determined by graphite furnace and flame atomic absorption spectrometry methods, respectively. The combined chelation therapy results show that Deferasirox and L(1) are able to remove cadmium ions from the body while iron concentration returned to the normal level and symptoms are also decreased.

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Section: Introductionmentioning

confidence: 99%

Chelation of cadmium by combining deferasirox and deferiprone in rats

et al. 2011

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“…9 LIC values derived from magnetic susceptometry as milligrams of iron per gram of liver tissue (wet weight) were multiplied by a factor of 3.33 to provide values per gram of liver tissue dry weight (mg Fe/g dw; the conventional units used for LIC). 10 Another technique used is a T2* imaging of heart. Low T2* values {< 8 ms compared with normal (> 20 ms)} are related to risk of heart failure and death in ironoverloaded thalassemia patients.…”

Section: Measurement Of Iron Overloadmentioning

confidence: 99%

Current status of iron overload and chelation with deferasirox

Choudhry

Naithani

2007

Indian J Pediatr

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A large number of complications in thalassemia major are due mainly to iron overload. Deferoxamine in iron-overloaded patients has established that chelation therapy, when given at an adequate dose, reduces iron-related complications. Parenteral administration and the daily nuisance of an infusion pump hinder the optimal compliance. Deferiprone is moderately effective oral iron chelator. Arthralgia and cytopenias constitute the main side effects. Deferasirox is a new orally effective iron chelator which has been shown to be non-inferior to deferoxamine in clinical trials. Further clinical trials especially in Indian children will tell if it stands the test of time.

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“…In agreement with the negative charge, [FeL 2 ] 3À is a slightly stronger base. Thus L 3À acts as tridentate coordinating ligand, where binding of the metal center occurs through the two phenolate groups and one of the nitrogen atoms of the heterocycle (Heinz et al, 1999).…”

Section: Introductionmentioning

confidence: 99%