2019. Lu X, Williams Z, Hards K, Tang J, Cheung CY, Aung HL, Wang B, Liu Z, Hu X, Lenaerts A, Woolhiser L, Hastings C, Zhang X, Wang Z, Rhee K, Ding K, Zhang T, Cook GM. Pyrazolo[1,5‑a]pyridine Inhibitor of the Respiratory Cytochrome bcc Complex for the Treatment of Drug-Resistant Tuberculosis.
2017. Presented at ASM Microbe. Tianyu Zhang, Xiaoyn Lu, Zhengchao Tu, Ke Ding, Xiantao Zhang.2017.Compound TB47 has strong activity against Mycobacterium tuberculosis both in vitro and in vivo. ASM MIcrobe Poster 41. Sunday.
Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciwences, Guangzhou, China. and EggBio Inc., Guangzhou, China
From poster - Results: TB47 had MIClux (μg/mL) 0.01−0.03 against autoluminescent Mtb H37Ra and 0.006 against Mtb H37Rv using MABA. Its IC50 against VERO was >100μM. Its MICs (μg/mL) against Mtb H37Rv using the agar method was 0.003, against autoluminescent 6 clinical drug-resistant isolates from China were 0.06-0.12 and against 5 single drug-resistant clinical isolates from USA were 0.0049 -0.0088μM. It showed good activity in the noninvasive murine model at 4mg/kg qd. An obvious relative light unit (RLU) reduction of the liv mice was observed, while RLU increased in the untreated group. In the aerosol infection model, all mice were healthy except for 4 of 5 untreated mice died between D26 and D28. The CFU counts (log10) were: TB47 (25mg/kg) , 5.86; INH, 2.49; INH-TB47, 2.92; PZA, 6.42; PZA-TB47, 2.47; RIF, 6.86; RIF-TB47, 1.83. TB47 showed very good synergetic bacteriocidal effect with RIF and PZA.
Chinese Academy of Sciences(CAS), State Key Laboratory of Respiratory Disease(SKLRD), Guangzhou City and the National Mega-project of China for Innovative Drugs.
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