Four component Ugi reaction based small-molecule probes for integrated phenotypic screening

Manikandan Thangaraj; Ksenia Lialin; Rambabu Dandela; Raju Adepu; Shimrit David; Meital Shema Mizrachi; Michael M. Meijler

doi:10.1016/j.bioorg.2024.107257

Four component Ugi reaction based small-molecule probes for integrated phenotypic screening

Manikandan Thangaraj, Ksenia Lialin, Rambabu Dandela, Raju Adepu, Shimrit David, Meital Shema Mizrachi, Michael M. Meijler

Department of Chemistry

Ben-Gurion University of the Negev

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

Abstract

Quorum-sensing (QS) is a cell density-dependent signaling pathway regulated by gene expression for intra- and interspecies communication. We have targeted QS activity in Pseudomonas aeruginosa, an opportunistic human pathogen that causes disease in immunocompromised patients, with a set of probes containing a variety of functional groups, including photoreactive (diazirine) and affinity (alkyne) moieties, that were synthesized using a four-component Ugi reaction (Ugi-4CR).

Original language	American English
Article number	107257
Journal	Bioorganic Chemistry
Volume	146
DOIs	https://doi.org/10.1016/j.bioorg.2024.107257
State	Published - 1 May 2024

Keywords

Multicomponent reactions (MCRs)
P. aeruginosa
Quorum sensing

All Science Journal Classification (ASJC) codes

Biochemistry
Molecular Biology
Drug Discovery
Organic Chemistry

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10.1016/j.bioorg.2024.107257

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title = "Four component Ugi reaction based small-molecule probes for integrated phenotypic screening",

abstract = "Quorum-sensing (QS) is a cell density-dependent signaling pathway regulated by gene expression for intra- and interspecies communication. We have targeted QS activity in Pseudomonas aeruginosa, an opportunistic human pathogen that causes disease in immunocompromised patients, with a set of probes containing a variety of functional groups, including photoreactive (diazirine) and affinity (alkyne) moieties, that were synthesized using a four-component Ugi reaction (Ugi-4CR).",

keywords = "Multicomponent reactions (MCRs), P. aeruginosa, Quorum sensing",

author = "Manikandan Thangaraj and Ksenia Lialin and Rambabu Dandela and Raju Adepu and Shimrit David and Mizrachi, \{Meital Shema\} and Meijler, \{Michael M.\}",

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year = "2024",

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doi = "10.1016/j.bioorg.2024.107257",

language = "American English",

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AU - Thangaraj, Manikandan

AU - Lialin, Ksenia

AU - Dandela, Rambabu

AU - Adepu, Raju

AU - David, Shimrit

AU - Mizrachi, Meital Shema

AU - Meijler, Michael M.

PY - 2024/5/1

Y1 - 2024/5/1

N2 - Quorum-sensing (QS) is a cell density-dependent signaling pathway regulated by gene expression for intra- and interspecies communication. We have targeted QS activity in Pseudomonas aeruginosa, an opportunistic human pathogen that causes disease in immunocompromised patients, with a set of probes containing a variety of functional groups, including photoreactive (diazirine) and affinity (alkyne) moieties, that were synthesized using a four-component Ugi reaction (Ugi-4CR).

AB - Quorum-sensing (QS) is a cell density-dependent signaling pathway regulated by gene expression for intra- and interspecies communication. We have targeted QS activity in Pseudomonas aeruginosa, an opportunistic human pathogen that causes disease in immunocompromised patients, with a set of probes containing a variety of functional groups, including photoreactive (diazirine) and affinity (alkyne) moieties, that were synthesized using a four-component Ugi reaction (Ugi-4CR).

KW - Multicomponent reactions (MCRs)

KW - P. aeruginosa

KW - Quorum sensing

UR - http://www.scopus.com/inward/record.url?scp=85187984239&partnerID=8YFLogxK

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DO - 10.1016/j.bioorg.2024.107257

M3 - Article

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SN - 0045-2068

VL - 146

JO - Bioorganic Chemistry

JF - Bioorganic Chemistry

M1 - 107257

ER -

Four component Ugi reaction based small-molecule probes for integrated phenotypic screening

Abstract

Keywords

All Science Journal Classification (ASJC) codes

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