Literature DB >> 20149497

Synthesis and evaluation of SQ109 analogues as potential anti-tuberculosis candidates.

Oluseye K Onajole1, Patrick Govender, Paul D van Helden, Hendrik G Kruger, Glenn E M Maguire, Ian Wiid, Thavendran Govender.   

Abstract

As part of an ongoing project to develop highly potent anti-tuberculosis therapeutics, six SQ109 derivatives were synthesized and screened in vitro for their anti-tuberculosis activity against the ATCC strain H37Rv and the extensively drug-resistant clinical strain XDR 173. Compound 16 with an extended alkene chain was the most active against both strains of Mycobacterium tuberculosis within a MIC range of 0.5-0.25 microM. Compound 12 and SQ109 were potent within a MIC range of 1-0.5 microM, whilst compound 18 displayed an activity within the MIC range of 0.5-2 microM against both Mycobacterium tuberculosis strains. Copyright (c) 2010 Elsevier Masson SAS. All rights reserved.

Entities:  

Mesh：

Substances：

Year:  2010        PMID： 20149497     DOI： 10.1016/j.ejmech.2010.01.046

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN： 0223-5234            Impact factor:   6.514


  8 in total

Review 1.  The chemical biology of new drugs in the development for tuberculosis.

Authors:  Clifton E Barry; John S Blanchard
Journal:  Curr Opin Chem Biol       Date:  2010-05-07       Impact factor: 8.822

Review 2.  New antituberculous drugs in development.

Authors:  Umesh G Lalloo; Anish Ambaram
Journal:  Curr HIV/AIDS Rep       Date:  2010-08       Impact factor: 5.071

Review 3.  Discovery and development of SQ109: a new antitubercular drug with a novel mechanism of action.

Authors:  Katherine A Sacksteder; Marina Protopopova; Clifton E Barry; Koen Andries; Carol A Nacy
Journal:  Future Microbiol       Date:  2012-07       Impact factor: 3.165

4.  Head-to-head prenyl tranferases: anti-infective drug targets.

Authors:  Fu-Yang Lin; Yi-Liang Liu; Kai Li; Rong Cao; Wei Zhu; Jordan Axelson; Ran Pang; Eric Oldfield
Journal:  J Med Chem       Date:  2012-05-01       Impact factor: 7.446

5.  N-(Adamantan-1-yl)-2-chloro-acetamide.

Authors:  Oluseye K Onajole; Thavendran Govender; Hendrik G Kruger; Glenn E M Maguire
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-05-20

6.  Recent developments in the epidemiology and management of tuberculosis - new solutions to old problems?

Authors:  Wolfgang M Thaiss; Cornelius C Thaiss; Christoph A Thaiss
Journal:  Infect Drug Resist       Date:  2012-01-09       Impact factor: 4.003

Review 7.  Recent Advances in the Synthesis of Polyamine Derivatives and Their Applications.

Authors:  Artemiy Nichugovskiy; Gian Cesare Tron; Mikhail Maslov
Journal:  Molecules       Date:  2021-10-30       Impact factor: 4.411

8.  MmpL3 as a Target for the Treatment of Drug-Resistant Nontuberculous Mycobacterial Infections.

Authors:  Wei Li; Amira Yazidi; Amitkumar N Pandya; Pooja Hegde; Weiwei Tong; Vinicius Calado Nogueira de Moura; E Jeffrey North; Jurgen Sygusch; Mary Jackson
Journal:  Front Microbiol       Date:  2018-07-10       Impact factor: 5.640
  8 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.