Literature DB >> 7837232

Synthesis and activity of some antimalarial bisquinolines.

K Raynes1, D Galatis, A F Cowman, L Tilley, L W Deady.   

Abstract

A new type of bisquinoline antimalarial, in which the basic side chain of chloroquine is retained, has been evaluated. Nine bisamides were prepared from aliphatic diacids with 6-amino- and 8-amino-((4-(diethylamino)-1-methylbutyl)amino)quinoline, and screened against chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro. The resistance indices for all compounds were lower than for chloroquine. The position of attachment and length of the linker chain markedly affected activity. The most active (IC50 = 120 nM against the chloroquine-resistant FAC8 strain) was the -(O)C(CH2)4C(O)- linked 8-amino compound.

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Year:  1995        PMID： 7837232     DOI： 10.1021/jm00001a026

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  8 in total

1.  Synthesis, antiprotozoal, antimicrobial, β-hematin inhibition, cytotoxicity and methemoglobin (MetHb) formation activities of bis(8-aminoquinolines).

Authors:  Kirandeep Kaur; Meenakshi Jain; Shabana I Khan; Melissa R Jacob; Babu L Tekwani; Savita Singh; Prati Pal Singh; Rahul Jain
Journal:  Bioorg Med Chem       Date:  2010-11-25       Impact factor: 3.641

2.  Specific inhibition of the eubacterial DNA ligase by arylamino compounds.

Authors:  G Ciarrocchi; D G MacPhee; L W Deady; L Tilley
Journal:  Antimicrob Agents Chemother       Date:  1999-11       Impact factor: 5.191

3.  Inhibition of the peroxidative degradation of haem as the basis of action of chloroquine and other quinoline antimalarials.

Authors:  P Loria; S Miller; M Foley; L Tilley
Journal:  Biochem J       Date:  1999-04-15       Impact factor: 3.857

4.  Potent Antimalarial Activity of Two Arenes Linked with Triamine Designed To Have Multiple Interactions with Heme.

Authors:  Yosuke Sakata; Kosuke Yabunaka; Yuko Kobayashi; Hirohisa Omiya; Naoki Umezawa; Hye-Sook Kim; Yusuke Wataya; Yoshimi Tomita; Yosuke Hisamatsu; Nobuki Kato; Hirokazu Yagi; Tadashi Satoh; Koichi Kato; Haruto Ishikawa; Tsunehiko Higuchi
Journal:  ACS Med Chem Lett       Date:  2018-09-24       Impact factor: 4.345

5.  In vitro activities of piperaquine and other 4-aminoquinolines against clinical isolates of Plasmodium falciparum in Cameroon.

Authors:  Leonardo K Basco; Pascal Ringwald
Journal:  Antimicrob Agents Chemother       Date:  2003-04       Impact factor: 5.191

6.  Identification of β-hematin inhibitors in a high-throughput screening effort reveals scaffolds with in vitro antimalarial activity.

Authors:  Rebecca D Sandlin; Kim Y Fong; Kathryn J Wicht; Holly M Carrell; Timothy J Egan; David W Wright
Journal:  Int J Parasitol Drugs Drug Resist       Date:  2014-09-11       Impact factor: 4.077

7.  Crystal structure and Hirshfeld surface analysis of N,N'-bis-(2-nitro-phen-yl)glutaramide.

Authors:  Akshatha R Salian; Sabine Foro; S Madan Kumar; B Thimme Gowda
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2018-09-21

8.  Acylated mono-, bis- and tris- cinchona-based amines containing ferrocene or organic residues: synthesis, structure and in vitro antitumor activity on selected human cancer cell lines.

Authors:  Benedek Imre Károlyi; Szilvia Bösze; Erika Orbán; Pál Sohár; László Drahos; Emese Gál; Antal Csámpai
Journal:  Molecules       Date:  2012-02-24       Impact factor: 4.411
  8 in total

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