Literature DB >> 23811093

Synthesis of 4-aminoquinoline-pyrimidine hybrids as potent antimalarials and their mode of action studies.

Kamaljit Singh1, Hardeep Kaur, Kelly Chibale, Jan Balzarini.   

Abstract

One of the most viable options to tackle the growing resistance to the antimalarial drugs such as artemisinin is to resort to synthetic drugs. The multi-target strategy involving the use of hybrid drugs has shown promise. In line with this, new hybrids of quinoline with pyrimidine have been synthesized and evaluated for their antiplasmodial activity against both CQ(S) and CQ(R) strains of Plasmodium falciparum. These depicted activity in nanomolar range and were found to bind to heme as well as AT rich pUC18 DNA.
Copyright © 2013 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  4-Aminoquinolines; Antimalarials; Drug discovery; Heme binding; Hybrid molecules

Mesh:

Substances:

Year:  2013        PMID: 23811093      PMCID: PMC7115683          DOI: 10.1016/j.ejmech.2013.05.046

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


  39 in total

1.  Preparation and antimalarial activities of "trioxaquines", new modular molecules with a trioxane skeleton linked to a 4-aminoquinoline.

Authors:  O Dechy-Cabaret; F Benoit-Vical; A Robert; B Meunier
Journal:  Chembiochem       Date:  2000-11-17       Impact factor: 3.164

2.  Spectroscopic studies on the thermodynamic and thermal denaturation of the ct-DNA binding of methylene blue.

Authors:  Endang Tri Wahyuni; Daryono H Tjahjono; Naoki Yoshioka; Hidenari Inoue
Journal:  Spectrochim Acta A Mol Biomol Spectrosc       Date:  2010-06-26       Impact factor: 4.098

3.  Synthesis and antimalarial activity of side chain modified 4-aminoquinoline derivatives.

Authors:  V Raja Solomon; W Haq; Kumkum Srivastava; Sunil K Puri; S B Katti
Journal:  J Med Chem       Date:  2007-01-25       Impact factor: 7.446

Review 4.  Intercalating drugs: DNA binding and molecular pharmacology.

Authors:  W D Wilson; R L Jones
Journal:  Adv Pharmacol Chemother       Date:  1981

5.  Design, synthesis and anti-plasmodial evaluation in vitro of new 4-aminoquinoline isatin derivatives.

Authors:  Idan Chiyanzu; Cailean Clarkson; Peter J Smith; Julie Lehman; Jiri Gut; Philip J Rosenthal; Kelly Chibale
Journal:  Bioorg Med Chem       Date:  2005-05-02       Impact factor: 3.641

6.  Discovery of dual function acridones as a new antimalarial chemotype.

Authors:  Jane X Kelly; Martin J Smilkstein; Reto Brun; Sergio Wittlin; Roland A Cooper; Kristin D Lane; Aaron Janowsky; Robert A Johnson; Rozalia A Dodean; Rolf Winter; David J Hinrichs; Michael K Riscoe
Journal:  Nature       Date:  2009-04-08       Impact factor: 49.962

7.  Chloroquine as intercalator: a hypothesis revived.

Authors:  S R Meshnick
Journal:  Parasitol Today       Date:  1990-03

Review 8.  Hybrid molecules with a dual mode of action: dream or reality?

Authors:  Bernard Meunier
Journal:  Acc Chem Res       Date:  2007-08-01       Impact factor: 22.384

9.  Malarial haemozoin/beta-haematin supports haem polymerization in the absence of protein.

Authors:  A Dorn; R Stoffel; H Matile; A Bubendorf; R G Ridley
Journal:  Nature       Date:  1995-03-16       Impact factor: 49.962

10.  Inhibition of human coronavirus 229E infection in human epithelial lung cells (L132) by chloroquine: involvement of p38 MAPK and ERK.

Authors:  Masakazu Kono; Koichiro Tatsumi; Alberto M Imai; Kengo Saito; Takayuki Kuriyama; Hiroshi Shirasawa
Journal:  Antiviral Res       Date:  2007-11-20       Impact factor: 5.970

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  3 in total

Review 1.  The Development of Novel Compounds Against Malaria: Quinolines, Triazolpyridines, Pyrazolopyridines and Pyrazolopyrimidines.

Authors:  Luiz C S Pinheiro; Lívia M Feitosa; Marilia O Gandi; Flávia F Silveira; Nubia Boechat
Journal:  Molecules       Date:  2019-11-13       Impact factor: 4.411

2.  Design and Synthesis of New Pyrimidine-Quinolone Hybrids as Novel hLDHA Inhibitors.

Authors:  Iván Díaz; Sofia Salido; Manuel Nogueras; Justo Cobo
Journal:  Pharmaceuticals (Basel)       Date:  2022-06-24

3.  Synthesis and anti-breast cancer evaluation of novel N-(guanidinyl)benzenesulfonamides.

Authors:  Mostafa M Ghorab; Marwa G El-Gazzar; Mansour S Alsaid
Journal:  Int J Mol Sci       Date:  2014-04-01       Impact factor: 5.923

  3 in total

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