Literature DB >> 23064162

The design, synthesis, in silico ADME profiling, antiplasmodial and antimycobacterial evaluation of new arylamino quinoline derivatives.

Matshawandile Tukulula1, Susan Little, Jiri Gut, Philip J Rosenthal, Baojie Wan, Scott G Franzblau, Kelly Chibale.   

Abstract

A series of new arylamino quinoline derivatives was designed based on the quinine and mefloquine scaffolds and evaluated in vitro for antiplasmodial and antimycobacterial activities. A number of these compounds exhibited significant activity against the drug-sensitive 3D7 and drug-resistant K1 strains of Plasmodium falciparum. Furthermore, two compounds, 4.12b and 4.12d, also showed 94 and 98% growth inhibitory activity against non-replicating and replicating Mycobacterium tuberculosis strains, respectively.
Copyright © 2012 Elsevier Masson SAS. All rights reserved.

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Year:  2012        PMID: 23064162     DOI: 10.1016/j.ejmech.2012.08.047

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


  4 in total

1.  Synthesis and antiplasmodial and antimycobacterial evaluation of new nitroimidazole and nitroimidazooxazine derivatives.

Authors:  Matshawandile Tukulula; Rajni-Kant Sharma; Maïa Meurillon; Aman Mahajan; Krupa Naran; Digby Warner; Jianxing Huang; Belew Mekonnen; Kelly Chibale
Journal:  ACS Med Chem Lett       Date:  2012-11-26       Impact factor: 4.345

2.  Synthesis and in vitro and in vivo pharmacological evaluation of new 4-aminoquinoline-based compounds.

Authors:  Matshawandile Tukulula; Mathew Njoroge; Efrem T Abay; Grace C Mugumbate; Lubbe Wiesner; Dale Taylor; Liezl Gibhard; Jennifer Norman; Kenneth J Swart; Jiri Gut; Philip J Rosenthal; Samuel Barteau; Judith Streckfuss; Jacques Kameni-Tcheudji; Kelly Chibale
Journal:  ACS Med Chem Lett       Date:  2013-10-01       Impact factor: 4.345

3.  New Quinoline-Urea-Benzothiazole Hybrids as Promising Antitubercular Agents: Synthesis, In Vitro Antitubercular Activity, Cytotoxicity Studies, and In Silico ADME Profiling.

Authors:  Rashmika Moodley; Chakes Mashaba; Goitsemodimo H Rakodi; Nomagugu B Ncube; Mabuatsela V Maphoru; Mohammed O Balogun; Audrey Jordan; Digby F Warner; Rene Khan; Matshawandile Tukulula
Journal:  Pharmaceuticals (Basel)       Date:  2022-05-05

Review 4.  Tetrazoles via Multicomponent Reactions.

Authors:  Constantinos G Neochoritis; Ting Zhao; Alexander Dömling
Journal:  Chem Rev       Date:  2019-02-01       Impact factor: 60.622

  4 in total

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