Literature DB >> 20537903

A new class of potential anti-tuberculosis agents: Synthesis and preliminary evaluation of novel acrylic acid ethyl ester derivatives.

M Shahjahan Kabir1, Ojas A Namjoshi, Ranjit Verma, Rebecca Polanowski, Sarah M Krueger, David Sherman, Marc A Rott, William R Schwan, Aaron Monte, James M Cook.   

Abstract

Novel acrylic acid ethyl ester derivatives were synthesized and evaluated as potential agents against Mycobacterium species. A versatile and efficient copper-catalyzed coupling process was developed and used to prepare a library of substituted acrylic acid ethyl ester analogs. Minimum inhibitory concentration assays indicated that two of these compounds 3 and 4 have greater in vitro activity against Mycobacterium smegmatis than rifampin, one of the current, first-line anti-mycobacterial chemotherapeutic agents. Moreover, members of this new class of compounds appear to exhibit a specific anti-mycobacterial effect and do not inhibit the growth of the other Gram-positive or Gram-negative species tested. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20537903     DOI： 10.1016/j.bmc.2010.05.016

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  5 in total

1.  Base-mediated stereospecific synthesis of aryloxy and amino substituted ethyl acrylates.

Authors:  M Shahjahan Kabir; Ojas A Namjoshi; Ranjit Verma; Michael Lorenz; V V N Phani Babu Tiruveedhula; Aaron Monte; Steven H Bertz; Alan W Schwabacher; James M Cook
Journal:  J Org Chem       Date:  2011-11-28       Impact factor: 4.354

2.  Syntheses and Biological Evaluations of Highly Functionalized Hydroxamate Containing and N-Methylthio Monobactams as Anti-Tuberculosis and β-Lactamase Inhibitory Agents.

Authors:  Mark W Majewski; Kyle D Watson; Sanghyun Cho; Patricia A Miller; Scott G Franzblau; Marvin J Miller
Journal:  Medchemcomm       Date:  2015-10-05       Impact factor: 3.597

3.  Design and synthesis of novel antimicrobials with activity against Gram-positive bacteria and mycobacterial species, including M. tuberculosis.

Authors:  V V N Phani Babu Tiruveedhula; Christopher M Witzigmann; Ranjit Verma; M Shahjahan Kabir; Marc Rott; William R Schwan; Sara Medina-Bielski; Michelle Lane; William Close; Rebecca L Polanowski; David Sherman; Aaron Monte; Jeffrey R Deschamps; James M Cook
Journal:  Bioorg Med Chem       Date:  2013-10-21       Impact factor: 3.641

4.  Stereoselective Direct N-Trifluoropropenylation of Heterocycles with a Hypervalent Iodonium Reagent.

Authors:  János T Csenki; Ádám Mészáros; Zsombor Gonda; Zoltán Novák
Journal:  Chemistry       Date:  2021-10-06       Impact factor: 5.020

5.  Short, Synthetic Cationic Peptides Have Antibacterial Activity against Mycobacterium smegmatis by Forming Pores in Membrane and Synergizing with Antibiotics.

Authors:  Kajal Gupta; Sameer Singh; Monique L van Hoek
Journal:  Antibiotics (Basel)       Date:  2015-08-24
  5 in total

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