Synthesis and In Vitro Antiprotozoan Evaluation of 4-/8-Aminoquinoline-based Lactams and Tetrazoles.

Aminoquinolines / chemical synthesis Antiprotozoal Agents / chemical synthesis Chemistry Techniques, Synthetic Lactams / chemistry Parasitic Sensitivity Tests Structure-Activity Relationship Tetrazoles / chemistry Trypanosoma brucei rhodesiense / drug effects
4-aminoquinoline β-lactams 8-aminoquinoline tetrazoles Plasmodium falciparum chloroquine multidrug-resistant (K1) strain aqueous kinetic solubility human African trypanosomiasis (HAT)

Journal

Molecules (Basel, Switzerland)
ISSN: 1420-3049
Titre abrégé: Molecules
Pays: Switzerland
ID NLM: 100964009

Informations de publication

Date de publication:
15 Dec 2020
Historique:
received: 02 11 2020
revised: 18 11 2020
accepted: 25 11 2020
entrez: 18 12 2020
pubmed: 19 12 2020
medline: 4 9 2021
Statut: epublish

Résumé

A second generation of 4-aminoquinoline- and 8-aminoquinoline-based tetrazoles and lactams were synthesized via the Staudinger and Ugi multicomponent reactions. These compounds were subsequently evaluated in vitro for their potential antiplasmodium activity against a multidrug-resistant K1 strain and for their antitrypanosomal activity against a cultured

Identifiants

DOI: 10.3390/molecules25245941 PMID: 33333924 PMC: PMC7765388
pubmed: 33333924
pii: molecules25245941
doi: 10.3390/molecules25245941
pmc: PMC7765388
pii:
doi:

Substances chimiques

Aminoquinolines 0
Antiprotozoal Agents 0
Lactams 0
Tetrazoles 0
4-aminoquinoline GTE5P5L97N
8-aminoquinoline U34EAV21TG

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Subventions

Organisme : National Research Foundation
ID : 116282

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Auteurs

Matshawandile Tukulula (M)

School of Chemistry and Physics, University of KwaZulu Natal, Durban 4000, South Africa.
ORCID: 0000-0002-1844-3614

Stefan Louw (S)

Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
Department of Chemistry and Biochemistry, University of Namibia, Windhoek 10005, Namibia.
ORCID: 0000-0002-3122-8812

Mathew Njoroge (M)

Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
ORCID: 0000-0003-1276-2224

Kelly Chibale (K)

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

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Classifications MeSH

questionsmedicales.fr › Composés hétérocycliques › Composés hétérocycliques à cycles fusionnés › Composés hétérobicycliques › Quinoléines › Aminoquinoléines › Synthesis and In Vitro Antiprotozoan...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Anti-infectieux › Antiparasitaires › Antiprotozoaires › Synthesis and In Vitro Antiprotozoan...
questionsmedicales.fr › Technologie, industrie et agriculture › Technologie › Technologie pharmaceutique › Techniques de chimie synthétique › Synthesis and In Vitro Antiprotozoan...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Lactames › Synthesis and In Vitro Antiprotozoan...
questionsmedicales.fr › Techniques d'investigation › Évaluation préclinique de médicament › Tests de sensibilité parasitaire › Synthesis and In Vitro Antiprotozoan...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Synthesis and In Vitro Antiprotozoan...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Azoles › Tétrazoles › Synthesis and In Vitro Antiprotozoan...
questionsmedicales.fr › Eucaryotes › Euglénozoaires › Kinetoplastida › Trypanosomatina › Trypanosoma › Trypanosoma brucei rhodesiense › Synthesis and In Vitro Antiprotozoan...