Screening of the open-access CRESTdb small-molecule library identified the imidazothiazole carboxamide sCQG200 (1) as an initial hit, with activity against H37Rv and Erdman Mycobacterium tuberculosis strains in cholesterol-containing medium (MIC90= 6.88 µM and 4.48 µM, respectively) and against intracellular Mtb (EC50=...
Leo Meng, David Grant, Han Xie et al.· bioRxiv· 0 citations
Rv1625c/Cya has emerged as a promising target for the development of treatment-shortening therapies for tuberculosis. Screening of an Enamine compound library identified sBQQ004 as an initial hit, and rapid hit optimization led to compound 1, which was subsequently confirmed as an Rv1625c/Cya agonist. Structure–activit...
Han Xie, Paridhi Sukheja, Kirsten T. Tolentino et al.· bioRxiv· 0 citations
COVID-19 highlighted the need for antivirals that can be rapidly deployed against both current and future coronavirus threats. CMX990 is a clinical stage coronavirus main protease (Mpro) inhibitor bearing a unique trifluoromethoxymethyl ketone warhead. Here, we broadly evaluate its pan-coronavirus target engagement, an...
N. G. R. Dayan Elshan, Karen C. Wolff, L. Riva et al.· bioRxiv· 0 citations
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