Identification of a Hit Series of Antileishmanial Compounds through the Use of Mixture-Based Libraries

Marc A. Giulianotti; Brian A. Vesely; Ala Azhari; Ashley Souza; Travis Lavoi; Richard A. Houghten; Dennis E. Kyle; James W. Leahy

doi:10.1021/acsmedchemlett.7b00045

Identification of a Hit Series of Antileishmanial Compounds through the Use of Mixture-Based Libraries

Marc A. Giulianotti
, Brian A. Vesely
, Ala Azhari
, Ashley Souza
, Travis Lavoi
, Richard A. Houghten
, Dennis E. Kyle
, James W. Leahy

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

6 Scopus citations

Abstract

From a screening campaign that included mixture-based libraries containing more than 6 million compounds, a lead series of bis-cyclic guanidines was identified as the most promising. Lead optimization resulted in the identification of potent (IC₅₀ < 500 nM) and selective compounds within this series as well as potent and selective monoguanidines.

Original language	English (US)
Pages (from-to)	802-807
Number of pages	6
Journal	ACS Medicinal Chemistry Letters
Volume	8
Issue number	8
DOIs	https://doi.org/10.1021/acsmedchemlett.7b00045
State	Published - Aug 10 2017
Externally published	Yes

Bibliographical note

Publisher Copyright:
© 2017 American Chemical Society.

Keywords

Leishmaniasis
lead optimization
mixture-based libraries
screening

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10.1021/acsmedchemlett.7b00045

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abstract = "From a screening campaign that included mixture-based libraries containing more than 6 million compounds, a lead series of bis-cyclic guanidines was identified as the most promising. Lead optimization resulted in the identification of potent (IC50 < 500 nM) and selective compounds within this series as well as potent and selective monoguanidines.",

keywords = "Leishmaniasis, lead optimization, mixture-based libraries, screening",

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doi = "10.1021/acsmedchemlett.7b00045",

language = "English (US)",

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AU - Giulianotti, Marc A.

AU - Vesely, Brian A.

AU - Azhari, Ala

AU - Souza, Ashley

AU - Lavoi, Travis

AU - Houghten, Richard A.

AU - Kyle, Dennis E.

AU - Leahy, James W.

PY - 2017/8/10

Y1 - 2017/8/10

N2 - From a screening campaign that included mixture-based libraries containing more than 6 million compounds, a lead series of bis-cyclic guanidines was identified as the most promising. Lead optimization resulted in the identification of potent (IC50 < 500 nM) and selective compounds within this series as well as potent and selective monoguanidines.

AB - From a screening campaign that included mixture-based libraries containing more than 6 million compounds, a lead series of bis-cyclic guanidines was identified as the most promising. Lead optimization resulted in the identification of potent (IC50 < 500 nM) and selective compounds within this series as well as potent and selective monoguanidines.

KW - Leishmaniasis

KW - lead optimization

KW - mixture-based libraries

KW - screening

UR - https://www.scopus.com/pages/publications/85027222273

UR - https://www.scopus.com/pages/publications/85027222273#tab=citedBy

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DO - 10.1021/acsmedchemlett.7b00045

M3 - Article

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EP - 807

JO - ACS Medicinal Chemistry Letters

JF - ACS Medicinal Chemistry Letters

IS - 8

ER -

Identification of a Hit Series of Antileishmanial Compounds through the Use of Mixture-Based Libraries

Abstract

Bibliographical note

Keywords

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