In Vitro: Antituberculosis agent-9 (Compound 5a; 48 h) shows cytotoxicity against HepG2 cells with an IC50 value of 3.1 μM. Antituberculosis agent-9 (6 days) also shows inhibitory activities against MRSA, M. abscessus and M. smegmatis with MICs of 4.0 μg/mL. Antituberculosis agent-9 (6 days) shows inhibitory activities against clinical isolates of M. tuberculosis with MICs of 0.5, 0.5, 0.5, 1.0 and 1.0 μg/mL for H37Rv, K4, K12, K5 and K16, respectively.
In Vivo: Antituberculosis agent-9 (Compound 5a; 300 mg/kg; oral; daily for 4 days) shows moderate antitubercular efficacy in mice.