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| Type |
Poster Presentation |
| Area |
Medicinal Chemistry |
| Room No. |
Grand Ballroom |
| Time |
10월 18일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-291 |
| Subject |
Discovery of novel anti-tubercular agent for the treatment of MDR/XDR TB |
| Authors |
Jung Hwan Choi, Youkyeong Song, Aram Lee, Guanghai Jin, Inhee Choi, Kaapjoo Park*
Medicinal Chemistry, Institut Pasteur Korea, Korea
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| Abstract |
Given the high attrition rate during clinical development and emergence of resistance, the discovery of additional antitubercular clinical candidates is clearly needed. There is still unmet medical need so discovering potent agents capable of reducing the treatment time of MDR/XDR TB patients with a success rate comparable to that of current therapies for drug-susceptible tuberculosis is in high demand as of today.
We have identified a novel scaffold, TTCA, which showed potent inhibitory activities against extracellular and intracellular bacteria. Around 360 derivatives of TTCA have been synthesized so far. Interestingly, TTCA compounds have better potency against intracellular bacteria. Also, TTCA compounds were active against tested clinical MDR strains with MIC less than 1uM. In vitro ADME and physicochemical properties profiling suggested that TTCA series have drug-like properties. In addition, TTCA series showed pharmacokinetic and safety profiles of druggable characteristics.
Herein, we report on finding of a novel TTCA scaffold that could effectively inhibit TB. Especially, TTCA compounds have the potentials to be developed as treatment for latent TB. Together, our data indicates that TTCA compounds are promising novel clinical candidates for the treatment of MDR/XDR TB.
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| E-mail |
junghwan.choi@ip-korea.org |
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122nd General Meeting of the KCS