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

50 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

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Keywords

antileishmanial agents
amastigote
benzodiazepine
pyrrolobenzodiazepine
bioengineering
paullone

Cite this

Clark, R. L., Carter, K. C., Mullen, A. B., Coxon, G. D., Owusu-Dapaah, G., McFarlane, E., ... Mackay, S. P. (2007). Identification of the benzodiazepines as a new class of antileishmanial agent. Bioorganic and Medicinal Chemistry Letters, 17(3), 624-627. https://doi.org/10.1016/j.bmcl.2006.11.004

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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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language = "English",

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Identification of the benzodiazepines as a new class of antileishmanial agent. / Clark, Rachael L.; Carter, Katharine C.; Mullen, Alexander B.; Coxon, Geoffrey D.; Owusu-Dapaah, George; McFarlane, Emma; Dao Duong Thi, M.; Grant, M.H.; Tettey, J.N.A.; Mackay, Simon P.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 17, No. 3, 02.2007, p. 624-627.

Research output: Contribution to journal › Article

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

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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.

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KW - amastigote

KW - benzodiazepine

KW - pyrrolobenzodiazepine

KW - bioengineering

KW - paullone

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DO - 10.1016/j.bmcl.2006.11.004

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EP - 627

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

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Access to Document

10.1016/j.bmcl.2006.11.004

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