Literature DB >> 11551771

Antiprotozoal and cytotoxicity evaluation of sulfonamide and urea analogues of quinacrine.

K Chibale1, H Haupt, H Kendrick, V Yardley, A Saravanamuthu, A H Fairlamb, S L Croft.   

Abstract

Sulfonamide and urea derivatives of quinacrine with varying methylene spacer lengths were synthesised and tested for inhibition of trypanothione reductase (TryR) and for activity in vitro against strains of the parasitic protozoa Trypanosoma, Leishmania, and Plasmodium. These derivatives are superior inhibitors of TryR relative to quinacrine with the best compound being 40 times more potent. Urea derivatives generally displayed good in vitro activity against all parasites.

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Year:  2001        PMID： 11551771     DOI： 10.1016/s0960-894x(01)00528-5

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


  14 in total

Review 1.  Parasite-specific trypanothione reductase as a drug target molecule.

Authors:  R Luise Krauth-Siegel; Oliver Inhoff
Journal:  Parasitol Res       Date:  2003-04-23       Impact factor: 2.289

2.  Two interacting binding sites for quinacrine derivatives in the active site of trypanothione reductase: a template for drug design.

Authors:  Ahilan Saravanamuthu; Tim J Vickers; Charles S Bond; Mark R Peterson; William N Hunter; Alan H Fairlamb
Journal:  J Biol Chem       Date:  2004-04-21       Impact factor: 5.157

3.  Leishmania amazonensis growth inhibitors: biological and theoretical features of sulfonamide 4-methoxychalcone derivatives.

Authors:  Alessandra M T Souza; Helena C Castro; Monique A Brito; Carla R Andrighetti-Fröhner; Uiaran Magalhães; Kely N Oliveira; Daniela Gaspar-Silva; Letícia K Pacheco; Antônio C Joussef; Mário Steindel; Cláudia M O Simões; Dilvani O Santos; Magaly G Albuquerque; Carlos R Rodrigues; Ricardo J Nunes
Journal:  Curr Microbiol       Date:  2009-07-23       Impact factor: 2.188

4.  Trypanothione reductase: a viable chemotherapeutic target for antitrypanosomal and antileishmanial drug design.

Authors:  M Omar F Khan
Journal:  Drug Target Insights       Date:  2007-06-19

5.  Acridine and acridinones: old and new structures with antimalarial activity.

Authors:  Aymé Fernández-Calienes Valdés
Journal:  Open Med Chem J       Date:  2011-03-09

Review 6.  Mini review on tricyclic compounds as an inhibitor of trypanothione reductase.

Authors:  Suresh Kumar; Md Rahmat Ali; Sandhya Bawa
Journal:  J Pharm Bioallied Sci       Date:  2014-10

7.  Room temperature synthesis and antibacterial activity of new sulfonamides containing n,n-diethyl-substituted amido moieties.

Authors:  Olayinka O Ajani; Oluwole B Familoni; Feipeng Wu; Johnbull O Echeme; Zheng Sujiang
Journal:  Int J Med Chem       Date:  2012-10-17

8.  Investigation of trypanothione reductase as a drug target in Trypanosoma brucei.

Authors:  Daniel Spinks; Emma J Shanks; Laura A T Cleghorn; Stuart McElroy; Deuan Jones; Daniel James; Alan H Fairlamb; Julie A Frearson; Paul G Wyatt; Ian H Gilbert
Journal:  ChemMedChem       Date:  2009-12       Impact factor: 3.466

9.  Identification of potent chemotypes targeting Leishmania major using a high-throughput, low-stringency, computationally enhanced, small molecule screen.

Authors:  Elizabeth R Sharlow; David Close; Tongying Shun; Stephanie Leimgruber; Robyn Reed; Gabriela Mustata; Peter Wipf; Jacob Johnson; Michael O'Neil; Max Grögl; Alan J Magill; John S Lazo
Journal:  PLoS Negl Trop Dis       Date:  2009-11-03

10.  Repurposing the anti-malarial drug, quinacrine: new anti-colitis properties.

Authors:  Alexander A Chumanevich; Erin E Witalison; Anusha Chaparala; Anastasiya Chumanevich; Prakash Nagarkatti; Mitzi Nagarkatti; Lorne J Hofseth
Journal:  Oncotarget       Date:  2016-08-16
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