Activity of Bisnaphthalimidopropyl Derivatives against Trypanosoma brucei

Antimicrobial Agents and Chemotherapy
Nuno A G GraçaAnabela Cordeiro-da-Silva

Abstract

Current treatments for African trypanosomiasis are either toxic, costly, difficult to administer, or prone to elicit resistance. This study evaluated the activity of bisnaphthalimidopropyl (BNIP) derivatives againstTrypanosoma brucei BNIPDiaminobutane (BNIPDabut), the most active of these compounds, showedin vitroinhibition in the single-unit nanomolar range, similar to the activity in the reference drug pentamidine, and presented low toxicity and adequate metabolic stability. Additionally, using a murine model of acute infection and live imaging, a significant decrease in parasite load in BNIPDabut-treated mice was observed. However, cure was not achieved. BNIPDabut constitutes a new scaffold for antitrypanosomal drugs that deserves further consideration.

References

Oct 22, 2002·The Journal of Pharmacology and Experimental Therapeutics·Fábio E MingattoAntonio C Santos
Aug 3, 2004·Nature Biotechnology·Sean R Eddy
May 3, 2005·International Journal for Parasitology·J TavaresA Cordeiro-da-Silva
Aug 5, 2008·Parasites & Vectors·Chris J Schofield, John P Kabayo
Nov 6, 2008·Chemico-biological Interactions·Lynda D RaltonPaul Kong Thoo Lin
Oct 17, 2009·Lancet·Reto BrunChristian Burri
Nov 26, 2009·ChemMedChem·Joana TavaresAnabela Cordeiro-da-Silva
Jan 13, 2010·European Journal of Medicinal Chemistry·Gemma A BarronPaul Kong Thoo Lin
Apr 26, 2011·Methods in Molecular Biology·Johan van MeerlooJacqueline Cloos
Jul 30, 2011·Toxicology in Vitro : an International Journal Published in Association with BIBRA·Shuguang WangJeffrey K Wickliffe
Aug 16, 2011·Cell Biology and Toxicology·Charles Stuart BestwickSusan J Duthie
Dec 14, 2011·Parasitology International·Joana TavaresAnabela Cordeiro-da-Silva
Mar 9, 2012·International Journal of Antimicrobial Agents·Sofia Costa LimaAnabela Cordeiro da Silva
Oct 15, 2013·Drug and Chemical Toxicology·Debojyoti BorkotokySubas C Parija
Oct 30, 2013·Drug and Chemical Toxicology·Rina TripathiChhagan N Patel
Nov 28, 2013·PLoS Neglected Tropical Diseases·Alex P McLatchieMartin C Taylor
May 27, 2014·Molecular and Biochemical Parasitology·David Horn
Aug 16, 2014·Clinical Epidemiology·Jose R FrancoJean G Jannin

❮ Previous
Next ❯

Citations

Aug 16, 2018·MedChemComm·Michael BerningerUlrike Holzgrabe
Jan 23, 2018·PLoS Neglected Tropical Diseases·Luís GasparAnabela Cordeiro-da-Silva

❮ Previous
Next ❯

Related Concepts

Related Feeds

African Trypanosomiasis

African trypanosomiasis, also known as sleeping sickness, is an insect-borne parasitic disease of humans and other animals. It is caused by protozoa of the species Trypanosoma brucei and almost invariably progresses to death unless treated. Discover the latest research on African trypanosomiasis here.

CRISPR Screens in Drug Resistance

CRISPR-Cas system enables the editing of genes to create or correct mutations. This feed focuses on the application of CRISPR-Cas system in high-throughput genome-wide screens to identify genes that may confer drug resistance.

Antiparasitics

Antiparasitics are medications which are indicated for the treatment of parasitic diseases. Discover the latest research on antiparasitics here.

Apoptosis

Apoptosis is a specific process that leads to programmed cell death through the activation of an evolutionary conserved intracellular pathway leading to pathognomic cellular changes distinct from cellular necrosis

Related Papers

Experimental Parasitology
Karin Merschjohann, Dietmar Steverding
Bioorganic & Medicinal Chemistry Letters
Yuxiang DongJonathan L Vennerstrom
Antimicrobial Agents and Chemotherapy
Njinkeng Joseph NkemnguDietmar Steverding
The Lancet Infectious Diseases
August StichUlrike Holzgrabe
© 2022 Meta ULC. All rights reserved