Synthesis of 2-substituted 9-oxa-guanines {5-aminooxazolo[5,4-d]pyrimidin-7(6H)-ones} and 9-oxa-2-thio-xanthines {5-mercaptooxazolo[5,4-d]pyrimidin-7(6H)-ones}
2008

Synthesis of 2-substituted 9-oxa-guanines and 9-oxa-2-thio-xanthines

publication Evidence: moderate

Author Information

Author(s): Mandal Subrata, Li Wen Tai, Bai Yan, Robertus Jon D, Kerwin Sean M

Primary Institution: University of Texas, Austin

Hypothesis

Can 2-substituted 5-aminooxazolo[5,4-d]pyrimidin-7(6H)-ones and related compounds inhibit ricin?

Conclusion

The study developed new routes to functionalized oxazolo[5,4-d]pyrimidines, with some compounds showing the ability to inhibit ricin.

Supporting Evidence

  • 5-aminooxazolo[5,4-d]pyrimidine-7(6H)-ones have been shown to inhibit ricin.
  • Two compounds prepared were found to inhibit ricin with IC50 ca. 1–3 mM.
  • Compounds 2b (IC50 = 2.8 mM) and 9 (IC50 = 1.6 mM) displayed some activity against ricin.

Takeaway

The researchers made new chemical compounds that might help stop a harmful protein called ricin from working.

Methodology

The study involved synthesizing various 2-substituted 5-aminooxazolo[5,4-d]pyrimidin-7(6H)-ones and evaluating their ability to inhibit ricin.

Limitations

The synthesis methods may not be suitable for all variations of the compounds.

Digital Object Identifier (DOI)

10.3762/bjoc.4.26

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