Literature DB >> 19054674

Chloroquine-astemizole hybrids with potent in vitro and in vivo antiplasmodial activity.

Chitalu C Musonda1, Gavin A Whitlock, Michael J Witty, Reto Brun, Marcel Kaiser.   

Abstract

A dual activity, conjugated approach has been taken to form hybrid molecules of two known antimalarial drugs, chloroquine (CQ) and the non-sedating H1 antagonist astemizole. A variety of linkers were investigated to conjugate the two agents into one molecule. Compounds 5-8 possessed improved in vitro activity against a CQ-resistant strain of Plasmodium falciparum, and examples 7 and 8 were active in vivo in mouse models of malaria.

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Year:  2008        PMID： 19054674     DOI： 10.1016/j.bmcl.2008.11.047

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


  7 in total

1.  A chemotype that inhibits three unrelated pathogenic targets: the botulinum neurotoxin serotype A light chain, P. falciparum malaria, and the Ebola filovirus.

Authors:  Igor Opsenica; James C Burnett; Rick Gussio; Dejan Opsenica; Nina Todorović; Charlotte A Lanteri; Richard J Sciotti; Montip Gettayacamin; Nicoletta Basilico; Donatella Taramelli; Jonathan E Nuss; Laura Wanner; Rekha G Panchal; Bogdan A Solaja; Sina Bavari
Journal:  J Med Chem       Date:  2011-01-25       Impact factor: 7.446

Review 2.  Are Antimalarial Hybrid Molecules a Close Reality or a Distant Dream?

Authors:  Drishti Agarwal; Rinkoo D Gupta; Satish K Awasthi
Journal:  Antimicrob Agents Chemother       Date:  2017-04-24       Impact factor: 5.191

3.  Structure-Activity Relationship Studies Reveal New Astemizole Analogues Active against Plasmodium falciparum In Vitro.

Authors:  Dickson Mambwe; Malkeet Kumar; Richard Ferger; Dale Taylor; Mathew Njoroge; Dina Coertzen; Janette Reader; Mariëtte van der Watt; Lyn-Marie Birkholtz; Kelly Chibale
Journal:  ACS Med Chem Lett       Date:  2021-08-02       Impact factor: 4.632

Review 4.  Reversed chloroquine molecules as a strategy to overcome resistance in malaria.

Authors:  David H Peyton
Journal:  Curr Top Med Chem       Date:  2012       Impact factor: 3.295

5.  Synthesis and Antileishmanial Evaluation of Arylimidamide-Azole Hybrids Containing a Phenoxyalkyl Linker.

Authors:  Ahmed Abdelhameed; Mei Feng; April C Joice; Emilia M Zywot; Yiru Jin; Chris La Rosa; Xiaoping Liao; Heidi L Meeds; Yena Kim; Junan Li; Craig A McElroy; Michael Zhuo Wang; Karl A Werbovetz
Journal:  ACS Infect Dis       Date:  2021-02-04       Impact factor: 5.578

6.  Asthma and atopic dermatitis are associated with increased risk of clinical Plasmodium falciparum malaria.

Authors:  Magali Herrant; Cheikh Loucoubar; Hubert Bassène; Bronner Gonçalves; Sabah Boufkhed; Fatoumata Diene Sarr; Arnaud Fontanet; Adama Tall; Laurence Baril; Odile Mercereau-Puijalon; Salaheddine Mécheri; Anavaj Sakuntabhai; Richard Paul
Journal:  BMJ Open       Date:  2013-07-24       Impact factor: 2.692

7.  Palladium-catalyzed amination of dichloroquinolines with adamantane-containing amines.

Authors:  Anton S Abel; Alexei D Averin; Olga A Maloshitskaya; Evgenii N Savelyev; Boris S Orlinson; Ivan A Novakov; Irina P Beletskaya
Journal:  Molecules       Date:  2013-02-06       Impact factor: 4.411
  7 in total

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