Discovery of halo-nitrobenzamides with potential application against human African trypanosomiasis

Jong Yeon Hwang; David Smithson; Michele Connelly; Julie Maier; Fangyi Zhu; Kiplin R. Guy

doi:10.1016/j.bmcl.2009.11.022

Discovery of halo-nitrobenzamides with potential application against human African trypanosomiasis

Jong Yeon Hwang, David Smithson, Michele Connelly, Julie Maier, Fangyi Zhu, Kiplin R. Guy

Research output: Contribution to journal › Article › peer-review

11 Scopus citations

Abstract

A series of halo-nitrobenzamide were synthesized and evaluated for their ability to block proliferation of Trypanosoma brucei brucei. A number of these compounds had significant activity against the parasite, particularly 2-chloro-N-(4-chlorophenyl)-5-nitrobenzamide 17 which exhibited low micromolar inhibitory potency against T. brucei and selectivity towards both malaria and mammalian cells.

Original language	English
Pages (from-to)	149-152
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	1
DOIs	https://doi.org/10.1016/j.bmcl.2009.11.022
State	Published - Jan 1 2010

Bibliographical note

Funding Information:
This work was supported by the American Lebanese Syrian Associated Charities (ALSAC) and St. Jude Children’s Research Hospital.

Keywords

HAT
Inhibitor
Trypanosomiasis

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.bmcl.2009.11.022

Cite this

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title = "Discovery of halo-nitrobenzamides with potential application against human African trypanosomiasis",

abstract = "A series of halo-nitrobenzamide were synthesized and evaluated for their ability to block proliferation of Trypanosoma brucei brucei. A number of these compounds had significant activity against the parasite, particularly 2-chloro-N-(4-chlorophenyl)-5-nitrobenzamide 17 which exhibited low micromolar inhibitory potency against T. brucei and selectivity towards both malaria and mammalian cells.",

keywords = "HAT, Inhibitor, Trypanosomiasis",

author = "Hwang, {Jong Yeon} and David Smithson and Michele Connelly and Julie Maier and Fangyi Zhu and Guy, {Kiplin R.}",

note = "Funding Information: This work was supported by the American Lebanese Syrian Associated Charities (ALSAC) and St. Jude Children{\textquoteright}s Research Hospital. ",

year = "2010",

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doi = "10.1016/j.bmcl.2009.11.022",

language = "English",

volume = "20",

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T1 - Discovery of halo-nitrobenzamides with potential application against human African trypanosomiasis

AU - Hwang, Jong Yeon

AU - Smithson, David

AU - Connelly, Michele

AU - Maier, Julie

AU - Zhu, Fangyi

AU - Guy, Kiplin R.

N1 - Funding Information: This work was supported by the American Lebanese Syrian Associated Charities (ALSAC) and St. Jude Children’s Research Hospital.

PY - 2010/1/1

Y1 - 2010/1/1

N2 - A series of halo-nitrobenzamide were synthesized and evaluated for their ability to block proliferation of Trypanosoma brucei brucei. A number of these compounds had significant activity against the parasite, particularly 2-chloro-N-(4-chlorophenyl)-5-nitrobenzamide 17 which exhibited low micromolar inhibitory potency against T. brucei and selectivity towards both malaria and mammalian cells.

AB - A series of halo-nitrobenzamide were synthesized and evaluated for their ability to block proliferation of Trypanosoma brucei brucei. A number of these compounds had significant activity against the parasite, particularly 2-chloro-N-(4-chlorophenyl)-5-nitrobenzamide 17 which exhibited low micromolar inhibitory potency against T. brucei and selectivity towards both malaria and mammalian cells.

KW - HAT

KW - Inhibitor

KW - Trypanosomiasis

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U2 - 10.1016/j.bmcl.2009.11.022

DO - 10.1016/j.bmcl.2009.11.022

M3 - Article

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AN - SCOPUS:72049103140

SN - 0960-894X

VL - 20

SP - 149

EP - 152

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 1

ER -

Discovery of halo-nitrobenzamides with potential application against human African trypanosomiasis

Abstract

Bibliographical note

Keywords

ASJC Scopus subject areas

UN SDGs

Access to Document

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