AI Article Synopsis
- Tuberculosis (TB), especially when combined with HIV and resistance to drugs, is a leading cause of global infectious disease deaths, highlighting the urgent need for new treatments.
- Recent research focused on creating new anti-TB compounds, specifically derivatives of 4-alkoxy cinnamic acid, which showed promising activity against Mycobacterium tuberculosis.
- One compound, identified as 13e, was significantly more effective than the standard drug isoniazid against drug-resistant TB strains and operates through a unique mechanism, indicating its potential for future drug development.
Article Abstract
Tuberculosis, HIV coinfection with TB, emergence of multidrug-resistant TB, and extensively drug-resistant TB are the major causes of death from infectious diseases worldwide. Because no new drug has been introduced in the last several decades, new classes of molecules as anti-TB drugs are urgently needed. Herein, we report the synthesis and structure-activity relationships of a series of thioester, amide, hydrazide, and triazolophthalazine derivatives of 4-alkoxy cinnamic acid. Many compounds exhibited submicromolar minimum inhibitory concentrations against Mycobacterium tuberculosis strain (H(37)Rv). Interestingly, compound 13e, a 4-isopentenyloxycinnamyl triazolophthalazine derivative, was found to be 100-1800 times more active than isoniazid (INH) when tested for its ability to inhibit the growth of INH-resistant M. tuberculosis strains. The results also revealed that 13e does not interfere with mycolic acid biosynthesis, thereby pointing to a different mode of action and representing an attractive lead compound for the development of new anti-TB agents.
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| http://dx.doi.org/10.1021/jm101510d | DOI Listing |
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