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Design, syntheses, and anti-tuberculosis activities of conjugates of piperazino-1,3-benzothiazin-4-ones (pBTZs) with 2,7-dimethylimidazo [1,2-a]pyridine-3-carboxylic acids and 7-phenylacetyl cephalosporins.
Majewski, Mark W; Tiwari, Rohit; Miller, Patricia A; Cho, Sanghyun; Franzblau, Scott G; Miller, Marvin J.
Afiliação
  • Majewski MW; Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, IN 46556, USA.
  • Tiwari R; Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, IN 46556, USA.
  • Miller PA; Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, IN 46556, USA.
  • Cho S; Institute for Tuberculosis Research, College of Pharmacy, MIC 964, Rm. 412, University of Illinois at Chicago, IL 60612, USA.
  • Franzblau SG; Institute for Tuberculosis Research, College of Pharmacy, MIC 964, Rm. 412, University of Illinois at Chicago, IL 60612, USA.
  • Miller MJ; Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, IN 46556, USA.
Bioorg Med Chem Lett ; 26(8): 2068-71, 2016 Apr 15.
Article em En | MEDLINE | ID: mdl-26951749
ABSTRACT
Tuberculosis (TB) remains one of the most threatening diseases in the world and the need for development of new therapies is dire. Herein we describe the rationale for the design and subsequent syntheses and studies of conjugates between pBTZ and both the imidazopyridine and cephalosporin scaffolds. Overall some compounds exhibited notable anti-TB activity in the range of 2-0.2 µM in the Microplate Alamar Blue (MABA) Assay.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Piperazinas / Piridinas / Tiazinas / Tuberculose / Desenho de Fármacos / Imidazóis / Mycobacterium tuberculosis / Antituberculosos Idioma: En Ano de publicação: 2016 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Piperazinas / Piridinas / Tiazinas / Tuberculose / Desenho de Fármacos / Imidazóis / Mycobacterium tuberculosis / Antituberculosos Idioma: En Ano de publicação: 2016 Tipo de documento: Article