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

Producción científica: Article › revisión exhaustiva

11 Citas (Scopus)

Resumen

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.

Idioma original	English
Páginas (desde-hasta)	149-152
Número de páginas	4
Publicación	Bioorganic and Medicinal Chemistry Letters
Volumen	20
N.º	1
DOI	https://doi.org/10.1016/j.bmcl.2009.11.022
Estado	Published - ene 1 2010

Nota bibliográfica

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

Financiación

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

Financiadores
St. Jude Children's Research Hospital
American Lebanese Syrian Associated Charities

ODS de las Naciones Unidas

Este resultado contribuye a los siguientes Objetivos de Desarrollo Sostenible

Good health and well being

ASJC Scopus subject areas

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

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10.1016/j.bmcl.2009.11.022

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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",

month = jan,

day = "1",

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

language = "English",

volume = "20",

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TY - JOUR

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

UR - https://www.scopus.com/pages/publications/72049103140

UR - https://www.scopus.com/pages/publications/72049103140#tab=citedBy

U2 - 10.1016/j.bmcl.2009.11.022

DO - 10.1016/j.bmcl.2009.11.022

M3 - Article

C2 - 19963377

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

Resumen

Nota bibliográfica

Financiación

ODS de las Naciones Unidas

ASJC Scopus subject areas

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