Cycloguanil

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Cycloguanil
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E number{{#property:P628}}
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Chemical and physical data
FormulaC11H14ClN5
Molar mass251.715 g/mol
3D model (JSmol)
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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

Cycloguanil is a dihydrofolate reductase inhibitor,[1] 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.[2] 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.[3]

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.[4]

References

  1. Srivastava IK, Vaidya AB; Vaidya (June 1999). "A mechanism for the synergistic antimalarial action of atovaquone and proguanil". Antimicrob. Agents Chemother. 43 (6): 1334–9. PMC 89274. PMID 10348748.
  2. PMID 6385887 (PMID 6385887)
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  3. PMID 15228254 (PMID 15228254)
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  4. PMID 8363372 (PMID 8363372)
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