Authors van der Westhuyzen, CW; Haynes, RK; Panayides, JL; Wiid, I; Parkinson, CJ in BENTHAM SCIENCE PUBL LTD published article about MYCOBACTERIUM-TUBERCULOSIS; CATALASE-PEROXIDASE; SUSCEPTIBILITY; ARTEMISININ; ANTIMALARIAL; RESISTANCE; KATG in [van der Westhuyzen, Christiaan W.; Panayides, Jenny-Lee] CSIR Biosci, ZA-0001 Pretoria, South Africa; [Haynes, Richard K.] North West Univ, Ctr Excellence Pharmaceut Sci, ZA-2531 Potchefstroom, South Africa; [Wiid, Ian] Stellenbosch Univ, SAMRC Ctr TB Res, DST NRF Ctr Excellence Biomed TB Res, Tygerberg, South Africa; [Parkinson, Christopher J.] Charles Sturt Univ, Sch Biomed Sci, Orange, NSW 2800, Australia in 2020, Cited 36. Formula: C5H4N2O2. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5
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 the incorporation of bacterial siderophores that results in the creation of antitubercular peroxidic leads for subsequent development as novel agents against tuberculosis. Methods: Eight novel peroxides were prepared and the antitubercular activity (H(37)Rv) 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.
Formula: C5H4N2O2. About Pyrazine-2-carboxylic acid, If you have any questions, you can contact van der Westhuyzen, CW; Haynes, RK; Panayides, JL; Wiid, I; Parkinson, CJ or concate me.
Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
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