Category: Professional Posters
Purpose: Our lab has developed novel indole-2-carboxamides with potent antimycobacterial activity both in vitro and in vivo against Mycobacterium tuberculosis and Mycobacterium abscessus. However, the indole-2-carboxamides suffer from poor bioavailability stemming from poor aqueous solubility. To improve aqueous solubility, we employed nonclassical bioisostere replacement of the indole-2-carboxamides amide linkage to a 1,2,4-oxadiazole.
Methods: This synthesis was achieved through a four-step synthesis. The antimycobacterial assessment against Mycobacterium tuberculosis and Mycobacterium abscessus was performed using microbroth dilution method.
Results: The oxadiazole ring was detrimental for Mycobacterium tuberculosis activity, however it does allow for bactericidal activity against Mycobacterium abscessus. The addition of a hydroxyl group on the N3 position improved activity against Mycobacterium abscessus and is bacteriostatic in nature.
Conclusion: The oxadiazole-based agents were proven to be effective in vitro against Mycobacterium abscessus but not Mycobacterium tuberculosis