Structure-Activity Relationship Studies Reveal New Astemizole Analogues Active against


Journal

ACS medicinal chemistry letters
ISSN: 1948-5875
Titre abrégé: ACS Med Chem Lett
Pays: United States
ID NLM: 101521073

Informations de publication

Date de publication:
12 Aug 2021
Historique:
received: 09 06 2021
accepted: 21 07 2021
entrez: 20 8 2021
pubmed: 21 8 2021
medline: 21 8 2021
Statut: epublish

Résumé

In the context of drug repositioning and expanding the existing structure-activity relationship around astemizole (AST), a new series of analogues were designed, synthesized, and evaluated for their antiplasmodium activity. Among 46 analogues tested, compounds

Identifiants

pubmed: 34413963
doi: 10.1021/acsmedchemlett.1c00328
pmc: PMC8366009
doi:

Types de publication

Journal Article

Langues

eng

Pagination

1333-1341

Informations de copyright

© 2021 American Chemical Society.

Déclaration de conflit d'intérêts

The authors declare no competing financial interest.

Références

Lancet Infect Dis. 2021 Aug;21(8):1120-1128
pubmed: 33864801
ChemMedChem. 2013 Nov;8(11):1795-804
pubmed: 24022991
ACS Med Chem Lett. 2012 Jan 25;3(3):216-21
pubmed: 24900457
Malar J. 2019 Mar 22;18(1):93
pubmed: 30902052
Bioorg Med Chem Lett. 2014 Feb 15;24(4):1085-8
pubmed: 24486132
Bioorg Med Chem. 2017 Dec 15;25(24):6332-6344
pubmed: 29042223
Bioorg Med Chem Lett. 2009 Jan 15;19(2):481-4
pubmed: 19054674
ACS Med Chem Lett. 2017 Sep 22;8(10):1019-1024
pubmed: 29057044
J Med Chem. 2010 Nov 25;53(22):7902-17
pubmed: 20804202
Infect Dis Clin North Am. 2004 Jun;18(2):171-88, table of contents
pubmed: 15145374
Bull N Y Acad Med. 1973 Aug;49(8):722-35
pubmed: 4580853
Nat Chem Biol. 2006 Aug;2(8):415-6
pubmed: 16816845
N Engl J Med. 2008 Dec 11;359(24):2619-20
pubmed: 19064625
ACS Infect Dis. 2019 Feb 8;5(2):303-315
pubmed: 30525439
Proc Natl Acad Sci U S A. 2012 May 29;109(22):8511-6
pubmed: 22586124
Am J Trop Med Hyg. 2007 Dec;77(6 Suppl):181-92
pubmed: 18165491

Auteurs

Dickson Mambwe (D)

Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.

Malkeet Kumar (M)

Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.

Richard Ferger (R)

Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.

Dale Taylor (D)

Drug Discovery and Development Centre (H3D), Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Observatory 7925, South Africa.

Mathew Njoroge (M)

Drug Discovery and Development Centre (H3D), Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Observatory 7925, South Africa.

Dina Coertzen (D)

Department of Biochemistry, Genetics & Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Private Bag X20, Hatfield, Pretoria 0028, South Africa.

Janette Reader (J)

Department of Biochemistry, Genetics & Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Private Bag X20, Hatfield, Pretoria 0028, South Africa.

Mariëtte van der Watt (M)

Department of Biochemistry, Genetics & Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Private Bag X20, Hatfield, Pretoria 0028, South Africa.

Lyn-Marie Birkholtz (LM)

Department of Biochemistry, Genetics & Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Private Bag X20, Hatfield, Pretoria 0028, South Africa.

Kelly Chibale (K)

Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
Drug Discovery and Development Centre (H3D), Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Observatory 7925, South Africa.
Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa.
South African Medical Research Council Drug Discovery and Development Research Unit, University of Cape Town, Rondebosch 7701, South Africa.

Classifications MeSH