Literature DB >> 26951749

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.

Mark W Majewski1, Rohit Tiwari1, Patricia A Miller1, Sanghyun Cho2, Scott G Franzblau2, Marvin J Miller1.   

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.
Copyright © 2016 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Benzothiazinones; Cephalosporin; Imidazopyridine; Tuberculosis

Mesh：

Substances：

Year:  2016        PMID： 26951749      PMCID： PMC4824297          DOI： 10.1016/j.bmcl.2016.02.076

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  23 in total

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Authors:  Neel R Gandhi; Paul Nunn; Keertan Dheda; H Simon Schaaf; Matteo Zignol; Dick van Soolingen; Paul Jensen; Jaime Bayona
Journal:  Lancet       Date:  2010-05-22       Impact factor: 79.321

Review 2.  Tuberculosis.

Authors:  Alimuddin Zumla; Mario Raviglione; Richard Hafner; C Fordham von Reyn
Journal:  N Engl J Med       Date:  2013-02-21       Impact factor: 91.245

Review 3.  Advances in the development of new tuberculosis drugs and treatment regimens.

Authors:  Alimuddin Zumla; Payam Nahid; Stewart T Cole
Journal:  Nat Rev Drug Discov       Date:  2013-05       Impact factor: 84.694

4.  Benzothiazinones are suicide inhibitors of mycobacterial decaprenylphosphoryl-β-D-ribofuranose 2'-oxidase DprE1.

Authors:  Claudia Trefzer; Henrieta Škovierová; Silvia Buroni; Adela Bobovská; Simone Nenci; Elisabetta Molteni; Florence Pojer; Maria R Pasca; Vadim Makarov; Stewart T Cole; Giovanna Riccardi; Katarína Mikušová; Kai Johnsson
Journal:  J Am Chem Soc       Date:  2011-12-21       Impact factor: 15.419

5.  Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity.

Authors:  Garrett C Moraski; Lowell D Markley; Philip A Hipskind; Helena Boshoff; Sanghyun Cho; Scott G Franzblau; Marvin J Miller
Journal:  ACS Med Chem Lett       Date:  2011-06-09       Impact factor: 4.345

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7.  Dual-action cephalosporins incorporating a 3'-tertiary-amine-linked quinolone.

Authors:  H A Albrecht; G Beskid; J G Christenson; K H Deitcher; N H Georgopapadakou; D D Keith; F M Konzelmann; D L Pruess; C C Wei
Journal:  J Med Chem       Date:  1994-02-04       Impact factor: 7.446

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Authors:  Benoit Lechartier; Ruben C Hartkoorn; Stewart T Cole
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Review 9.  Comprehensive analysis of methods used for the evaluation of compounds against Mycobacterium tuberculosis.

Authors:  Scott G Franzblau; Mary Ann DeGroote; Sang Hyun Cho; Koen Andries; Eric Nuermberger; Ian M Orme; Khisimuzi Mdluli; Iñigo Angulo-Barturen; Thomas Dick; Veronique Dartois; Anne J Lenaerts
Journal:  Tuberculosis (Edinb)       Date:  2012-08-30       Impact factor: 3.131

10.  PA-824 kills nonreplicating Mycobacterium tuberculosis by intracellular NO release.

Authors:  Ramandeep Singh; Ujjini Manjunatha; Helena I M Boshoff; Young Hwan Ha; Pornwaratt Niyomrattanakit; Richard Ledwidge; Cynthia S Dowd; Ill Young Lee; Pilho Kim; Liang Zhang; Sunhee Kang; Thomas H Keller; Jan Jiricek; Clifton E Barry
Journal:  Science       Date:  2008-11-28       Impact factor: 63.714
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  3 in total

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Journal:  RSC Med Chem       Date:  2022-03-10

2.  Quinolone-isoniazid hybrids: synthesis and preliminary in vitro cytotoxicity and anti-tuberculosis evaluation.

Authors:  Richard M Beteck; Ronnett Seldon; Audrey Jordaan; Digby F Warner; Heinrich C Hoppe; Dustin Laming; Lesetja J Legoabe; Setshaba D Khanye
Journal:  Medchemcomm       Date:  2019-01-11       Impact factor: 3.597

3.  8-cyanobenzothiazinone analogs with potent antitubercular activity.

Authors:  Gang Zhang; Li Sheng; Pooja Hegde; Yan Li; Courtney C Aldrich
Journal:  Med Chem Res       Date:  2021-01-13       Impact factor: 1.965
  3 in total

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