Full Text Inquiry
ePub [ahead of print] Inquiry Form:

Thank you for your interest in the full text of this ePub article. The full text of this article is not available as yet. Could you please complete and submit the brief EPub full text inquiry form given below and one of our representatives will contact you shortly with details of the article, it's availability, and price on order.

Article Detail:

Anti-Mycobacterial Peroxides: A New Class of Agents for Development Against Tuberculosis

Background: With few exceptions, existing tuberculosis drugs were developed many years ago and resistance profiles have emerged. This has created a need for new drugs with discrete modes of action. There is evidence that tuberculosis (like other bacteria) is susceptible to oxidative pressure and this has yet to be properly utilised as a therapeutic approach in a manner similar to that which has proven highly successful in malaria therapy.

Objective: To develop an alternative approach to incorporation of bacterial siderophores that results in creation of antitubercular peroxidic leads for subsequent development as novel agents against tuberculosis.

Methods: Eight novel peroxides were prepared and the antitubercular activity (H37Rv) was compared to existing artemisinin derivatives in vitro. The potential for toxicity was evaluated against the L6 rat skeletal myoblast and HeLa cervical cancer lines in vitro.

Results: The addition of a pyrimidinyl residue to an artemisinin or, preferably, a tetraoxane peroxidic structure results in antitubercular activity in vitro. The same effect is not observed in the absence of the pyrimidine or with other heteroaromatic substituents.

Conclusion: The incorporation of a pyrimidinyl residue adjacent to the peroxidic function in an organic peroxide results in anti-tubercular activity in an otherwise inactive peroxidic compound. This will be a useful approach for creating oxidative drugs to target tuberculosis.

Journal Title: Medicinal Chemistry

Price: $95

Inquiry Form

13 + 2 =
Solve this simple math problem and enter the result. E.g. for 1+3, enter 4.