Optimization and Evaluation of 5‐Styryl‐Oxathiazol‐2‐one Mycobacterium tuberculosis Proteasome Inhibitors as Potential Antitubercular Agents

• Published in: ChemistryOpen (Weinheim) Vol. 4; no. 3; pp. 342 - 362
• Main Authors: Russo, Francesco, Gising, Johan, Åkerbladh, Linda, Roos, Annette K., Naworyta, Agata, Mowbray, Sherry L., Sokolowski, Anders, Henderson, Ian, Alling, Torey, Bailey, Mai A., Files, Megan, Parish, Tanya, Karlén, Anders, Larhed, Mats
• Format: Journal Article
• Language: English
• Published: Germany John Wiley & Sons, Inc 01.06.2015; John Wiley & Sons, Ltd
• Subjects: 5-styryl-oxathiazolones; antitubercular agents; Bacteria; Drugs; Human; Inhibitors; Mtb proteasome inhibitor; Mycobacterium tuberculosis; nonreplicating Mtb; Optimization; rapid bactericidal activity; Selectivity; Therapy; Tuberculosis; antitubercular agents; nonreplicating Mtb; Mycobacterium tuberculosis; 5-styryl-oxathiazolones; Mtb proteasome inhibitor; rapid bactericidal activity

This is the first report of 5‐styryl‐oxathiazol‐2‐ones as inhibitors of the Mycobacterium tuberculosis (Mtb) proteasome. As part of the study, the structure–activity relationship of oxathiazolones as Mtb proteasome inhibitors has been investigated. Furthermore, the prepared compounds displayed a goo...