Whole-cell based high-throughput screen with aerobically grown Mtb H37Rv. IC50 = 0.19 mM, MIC = 0.09 mM, In vivo active in mouse models. From Abstract: "In multiple mouse models of TB infection, TAM16 showed in vivo efficacy equal to the first-line TB drug isoniazid, both as a monotherapy and in combination therapy with rifampicin. TAM16 has excellent pharmacological and safety profiles, and the frequency of resistance for TAM16 is 100-fold lower than INH, suggesting that it can be developed as a new antitubercular aimed at the acute infection."
PKS13 Inhibitors - TAM16