Discovery of thienothiazolocarboxamide analogues as novel anti-tubercular agent

Jin, Guang‐Zhen; Kim, Young Mi; Lee, Aram; Choi, Jung‐Hwan; Kang, Sunhee; Seo, Mooyoung; Seo, Jeong Jea; Lee, Sumi; Kang, Ju‐Hee; Kim, Jaeseung; Park, Sinyoung; Woo, Minjeong; Falcão, Virgínia Carla de Almeida; Lee, Honggun; Heo, Jinyeong; Shum, David; Park, Kaapjoo; Delorme, Vincent; Choi, Inhee

doi:10.1016/j.bmc.2020.115797

Cited by 4 publications

(2 citation statements)

References 10 publications

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“…Jin et al reported thienothiazole amide derivative 120 (Figure 15) as an exciting new anti-TB lead, which they obtained by optimizing the HTS hit 119 (Figure 15). 283 Compound 120 displayed good activity against Mtb H37Rv expressing green fluorescent protein (GFP), both in broth and in macrophages (MIC 50 values 0.76 and 0.19 μM, respectively), and against a panel of MDR clinical isolates (MICs 2−4 μM). It also showed no cytotoxicity toward HepG2 cells (CC 50 > 50 μM) and modest inhibition of hERG (IC 50 28 μM) and CYPs 3A4, 2D6, and 2C9 (IC 50 s ∼ 7 μM).…”

Section: Compounds Targeting Cell Wallmentioning

confidence: 99%

Tuberculosis Drug Discovery: Challenges and New Horizons

et al. 2022

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Over the past 2000 years, tuberculosis (TB) has claimed more lives than any other infectious disease. In 2020 alone, TB was responsible for 1.5 million deaths worldwide, comparable to the 1.8 million deaths caused by COVID-19. The World Health Organization has stated that new TB drugs must be developed to end this pandemic. After decades of neglect in this field, a renaissance era of TB drug discovery has arrived, in which many novel candidates have entered clinical trials. However, while hundreds of molecules are reported annually as promising anti-TB agents, very few successfully progress to clinical development. In this Perspective, we critically review those anti-TB compounds published in the last 6 years that demonstrate good in vivo efficacy against Mycobacterium tuberculosis. Additionally, we highlight the main challenges and strategies for developing new TB drugs and the current global pipeline of drug candidates in clinical studies to foment fresh research perspectives.

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Section: Compounds Targeting Cell Wallmentioning

confidence: 99%

Tuberculosis Drug Discovery: Challenges and New Horizons

et al. 2022

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“…These compounds and their derivatives have a good antibacterial potential activity [14], and their structure is essential part of many compounds used frequently in pharmaceutical treatment [15]. Generally, this propriety is due to their low-risk for the human body [16,17].…”

Section: Introductionmentioning

confidence: 99%