Lerisetron Analogues with Antimalarial Properties: Synthesis, Structure-Activity Relationship Studies, and Biological Assessment.


Journal

ACS omega
ISSN: 2470-1343
Titre abrégé: ACS Omega
Pays: United States
ID NLM: 101691658

Informations de publication

Date de publication:
31 Mar 2020
Historique:
received: 23 01 2020
accepted: 05 03 2020
entrez: 8 4 2020
pubmed: 8 4 2020
medline: 8 4 2020
Statut: epublish

Résumé

A phenotypic whole cell high-throughput screen against the asexual blood and liver stages of the malaria parasite identified a benzimidazole chemical series. Among the hits were the antiemetic benzimidazole drug Lerisetron

Identifiants

pubmed: 32258933
doi: 10.1021/acsomega.0c00327
pmc: PMC7114883
doi:

Types de publication

Journal Article

Langues

eng

Pagination

6967-6982

Informations de copyright

Copyright © 2020 American Chemical Society.

Déclaration de conflit d'intérêts

The authors declare no competing financial interest.

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Auteurs

Rudolf Mueller (R)

Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.

Virsinha Reddy (V)

Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.

Aloysius T Nchinda (AT)

Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.

Fanuel Mebrahtu (F)

Drug Discovery and Development Centre (H3D), 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.

Nina Lawrence (N)

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

Lloyd Tanner (L)

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

Marine Barnabe (M)

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

Charles J Eyermann (CJ)

Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.

Bin Zou (B)

Shanghai Blueray Biopharma Co. LTD, Block 3, 576 Libing Road, Pudong New District, Shanghai 201301, China.

Ravinder R Kondreddi (RR)

PJS Pharma Pvt. Ltd., Plot No. 103/1, Phase II, IDA Cherlapally, Hyderabad 500051, India.

Suresh B Lakshminarayana (SB)

Novartis Institute for Tropical Diseases, 5300 Chiron Way, Emeryville, California 94608, United States.

Matthias Rottmann (M)

Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, CH-4051 Basel, Switzerland.
University of Basel, 4002 Basel, Switzerland.

Leslie J Street (LJ)

Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.

Kelly Chibale (K)

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

Classifications MeSH