Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 151, Issue -, Pages 1-8Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2018.03.060
Keywords
Benzothiazionones; PBTZ169; Antimycobacterial activity; Synthesis
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Funding
- National Mega-project for Innovative Drugs [2017ZX09201001, 2015ZX09102007-008, 2015ZX09304006-016]
- CAMS Initiative for Innovative Medicine [2016-I2M-1-010]
- CAMS Innovation Fund for Medical Science [CAMS-2017-I2M-1-011]
- PUMC Youth Fund [2017350011]
- Beijing Municipal Administration of Hospitals Clinical Medicine Development of Special Funding Support [ZYLX201304]
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We herein report the design and synthesis of benzothiazinones containing a piperidine moiety as new antitubercular agents based on the structure feature of IMB-ZR-1 discovered in our lab. Some of them were found to have good in vitro activity (MIC < 1 mu g/mL) against drug-susceptible Mycobacterium tuberculosis H37RV strain. After two set of modifications, compound 2i were found to display comparable in vitro anti-TB activity (MIC < 0.016 mu g/mL) to PBTZ169 against drug-sensitive and resistant mycobacterium tuberculosis strains. Compound 2i also showed acceptable PK profiles. Studies to determine PK profiles in lung and in vivo efficacy of 21 are currently under way. (C) 2018 Elsevier Masson SAS. All rights reserved.
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