Identification of the benzodiazepines as a new class of antileishmanial agent

Rachael L. Clark; Katharine C. Carter; Alexander B. Mullen; Geoffrey D. Coxon; George Owusu-Dapaah; Emma McFarlane; M. Dao Duong Thi; M.H. Grant; J.N.A. Tettey; Simon P. Mackay

doi:10.1016/j.bmcl.2006.11.004

Identification of the benzodiazepines as a new class of antileishmanial agent

Rachael L. Clark, Katharine C. Carter, Alexander B. Mullen, Geoffrey D. Coxon, George Owusu-Dapaah, Emma McFarlane, M. Dao Duong Thi, M.H. Grant, J.N.A. Tettey, Simon P. Mackay

Strathclyde Institute Of Pharmacy And Biomedical Sciences

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

57 Citations (Scopus)

Abstract

The continual increase in drug resistance; the lack of new chemotherapeutic agents; the toxicity of existing agents and the increasing morbidity with HIV co-infection mean the search for new antileishmanial agents has never been more urgent. We have identified the benzodiazepines as a structural class for antileishmanial hit optimisation, and demonstrated that their in vitro activity is comparable with the clinically used drug, sodium stibogluconate, and that the compounds are not toxic to macrophages.

Original language	English
Pages (from-to)	624-627
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	17
Issue number	3
DOIs	https://doi.org/10.1016/j.bmcl.2006.11.004
Publication status	Published - Feb 2007

Keywords

antileishmanial agents
amastigote
benzodiazepine
pyrrolobenzodiazepine
bioengineering
paullone

UN SDGs

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

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10.1016/j.bmcl.2006.11.004

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title = "Identification of the benzodiazepines as a new class of antileishmanial agent",

abstract = "The continual increase in drug resistance; the lack of new chemotherapeutic agents; the toxicity of existing agents and the increasing morbidity with HIV co-infection mean the search for new antileishmanial agents has never been more urgent. We have identified the benzodiazepines as a structural class for antileishmanial hit optimisation, and demonstrated that their in vitro activity is comparable with the clinically used drug, sodium stibogluconate, and that the compounds are not toxic to macrophages.",

keywords = "antileishmanial agents, amastigote, benzodiazepine, pyrrolobenzodiazepine, bioengineering, paullone",

author = "Clark, {Rachael L.} and Carter, {Katharine C.} and Mullen, {Alexander B.} and Coxon, {Geoffrey D.} and George Owusu-Dapaah and Emma McFarlane and {Dao Duong Thi}, M. and M.H. Grant and J.N.A. Tettey and Mackay, {Simon P.}",

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doi = "10.1016/j.bmcl.2006.11.004",

language = "English",

volume = "17",

pages = "624--627",

journal = "Bioorganic and Medicinal Chemistry Letters",

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TY - JOUR

T1 - Identification of the benzodiazepines as a new class of antileishmanial agent

AU - Clark, Rachael L.

AU - Carter, Katharine C.

AU - Mullen, Alexander B.

AU - Coxon, Geoffrey D.

AU - Owusu-Dapaah, George

AU - McFarlane, Emma

AU - Dao Duong Thi, M.

AU - Grant, M.H.

AU - Tettey, J.N.A.

AU - Mackay, Simon P.

PY - 2007/2

Y1 - 2007/2

N2 - The continual increase in drug resistance; the lack of new chemotherapeutic agents; the toxicity of existing agents and the increasing morbidity with HIV co-infection mean the search for new antileishmanial agents has never been more urgent. We have identified the benzodiazepines as a structural class for antileishmanial hit optimisation, and demonstrated that their in vitro activity is comparable with the clinically used drug, sodium stibogluconate, and that the compounds are not toxic to macrophages.

AB - The continual increase in drug resistance; the lack of new chemotherapeutic agents; the toxicity of existing agents and the increasing morbidity with HIV co-infection mean the search for new antileishmanial agents has never been more urgent. We have identified the benzodiazepines as a structural class for antileishmanial hit optimisation, and demonstrated that their in vitro activity is comparable with the clinically used drug, sodium stibogluconate, and that the compounds are not toxic to macrophages.

KW - antileishmanial agents

KW - amastigote

KW - benzodiazepine

KW - pyrrolobenzodiazepine

KW - bioengineering

KW - paullone

UR - http://dx.doi.org/10.1016/j.bmcl.2006.11.004

U2 - 10.1016/j.bmcl.2006.11.004

DO - 10.1016/j.bmcl.2006.11.004

M3 - Article

SN - 0960-894X

VL - 17

SP - 624

EP - 627

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 3

ER -

Identification of the benzodiazepines as a new class of antileishmanial agent

Abstract

Keywords

UN SDGs

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