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Cycloguanil is a dihydrofolate reductase inhibitor, and is a metabolite of the antimalarial drug proguanil; its formation in vivo has been thought to be primarily responsible for the antimalarial activity of proguanil. However, more recent work has indicated that, while proguanil is synergistic with the drug atovaquone (as in the combination Malarone), cycloguanil is in fact antagonistic to the effects of atovaquone, suggesting that, unlike cycloguanil, proguanil may have an alternative mechanism of antimalarial action besides dihydrofolate reductase inhibition.

AttributesValues
rdf:type
rdfs:label
  • سيكلوجوانيل (ar)
  • Cycloguanil (en)
  • Cicloguanil (it)
rdfs:comment
  • سيكلوجوانيل (بالإنجليزية: Cycloguanil) هو مثبط مختزلة ثنائي الهيدروفولات، وهو مستقلب لعقار بروغوانيل المضاد للملاريا. يُعتقد أن تكوينه في الجسم الحي هو المسؤول الأول عن نشاط البروغوانيل المضاد للملاريا. على الرغم من أن السيكلوجوانيل لا يستخدم حاليًا بشكل عام كمضاد للملاريا، فقد أدى التطور المستمر للمقاومة للأدوية المضادة للملاريا الحالية إلى تجديد الاهتمام بدراسة استخدام سيكلوجوانيل مع أدوية أخرى. (ar)
  • Cycloguanil is a dihydrofolate reductase inhibitor, and is a metabolite of the antimalarial drug proguanil; its formation in vivo has been thought to be primarily responsible for the antimalarial activity of proguanil. However, more recent work has indicated that, while proguanil is synergistic with the drug atovaquone (as in the combination Malarone), cycloguanil is in fact antagonistic to the effects of atovaquone, suggesting that, unlike cycloguanil, proguanil may have an alternative mechanism of antimalarial action besides dihydrofolate reductase inhibition. (en)
  • Il cicloguanil è un metabolita attivo del proguanil, un farmaco antimalarico, ed un inibitore della diidrofolato reduttasi. Si ritiene che la sua formazione in vivo possa essere il principale responsabile per l'attività antimalarica del proguanil. Tuttavia, studi più recenti hanno indicato che, mentre il proguanil è sinergico con l'atovaquone (come nella combinazione Malarone), il cicloguanil è infatti antagonista agli effetti dell'atovaquone, suggerendo che, a differenza del cicloguanil, il proguanil può avere un meccanismo alternativo nell'azione antimalarica oltre all'inibizione della diidrofolato reduttasi. (it)
foaf:depiction
  • http://commons.wikimedia.org/wiki/Special:FilePath/Cycloguanil.svg
  • http://commons.wikimedia.org/wiki/Special:FilePath/Cycloguanil_synthesis.svg
  • http://commons.wikimedia.org/wiki/Special:FilePath/cycloguanil_sf.png
dcterms:subject
Wikipage page ID
Wikipage revision ID
Link from a Wikipage to another Wikipage
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dbp:wikiPageUsesTemplate
thumbnail
ATC suffix
  • BB02 (en)
ATC prefix
  • P01 (en)
c
CAS number
ChEMBL
ChemSpiderID
Cl
H
image
  • cycloguanil_sf.png (en)
IUPAC name
n
PubChem
SMILES
  • Clc1cccN2C\N (en)
StdInChI
StdInChIKey
  • QMNFFXRFOJIOKZ-UHFFFAOYSA-N (en)
UNII
verifiedrevid
Watchedfields
  • changed (en)
has abstract
  • سيكلوجوانيل (بالإنجليزية: Cycloguanil) هو مثبط مختزلة ثنائي الهيدروفولات، وهو مستقلب لعقار بروغوانيل المضاد للملاريا. يُعتقد أن تكوينه في الجسم الحي هو المسؤول الأول عن نشاط البروغوانيل المضاد للملاريا. على الرغم من أن السيكلوجوانيل لا يستخدم حاليًا بشكل عام كمضاد للملاريا، فقد أدى التطور المستمر للمقاومة للأدوية المضادة للملاريا الحالية إلى تجديد الاهتمام بدراسة استخدام سيكلوجوانيل مع أدوية أخرى. (ar)
  • Cycloguanil is a dihydrofolate reductase inhibitor, and is a metabolite of the antimalarial drug proguanil; its formation in vivo has been thought to be primarily responsible for the antimalarial activity of proguanil. However, more recent work has indicated that, while proguanil is synergistic with the drug atovaquone (as in the combination Malarone), cycloguanil is in fact antagonistic to the effects of atovaquone, suggesting that, unlike cycloguanil, proguanil may have an alternative mechanism of antimalarial action besides dihydrofolate reductase inhibition. Although cycloguanil is not currently in general use as an antimalarial, the continuing development of resistance to current antimalarial drugs has led to renewed interest in studying the use of cycloguanil in combination with other drugs. (en)
  • Il cicloguanil è un metabolita attivo del proguanil, un farmaco antimalarico, ed un inibitore della diidrofolato reduttasi. Si ritiene che la sua formazione in vivo possa essere il principale responsabile per l'attività antimalarica del proguanil. Tuttavia, studi più recenti hanno indicato che, mentre il proguanil è sinergico con l'atovaquone (come nella combinazione Malarone), il cicloguanil è infatti antagonista agli effetti dell'atovaquone, suggerendo che, a differenza del cicloguanil, il proguanil può avere un meccanismo alternativo nell'azione antimalarica oltre all'inibizione della diidrofolato reduttasi. Anche se cicloguanil non è attualmente in uso generale come antimalarico, il continuo sviluppo della resistenza ai farmaci antimalarici ha portato ad un rinnovato interesse per lo studio di esso in combinazione con altri farmaci. (it)
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prov:wasDerivedFrom
page length (characters) of wiki page
CAS number
  • 516-21-2
ChEMBL
  • 747
FDA UNII code
  • 26RM326WVN
PubChem
  • 9049
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