Synthesis of pyrimidine and quinolone conjugates as a scaffold for dual inhibitors of HIV reverse transcriptase and integrase

Zhengqiang Wang; Robert Vince

doi:10.1016/j.bmcl.2008.01.025

Synthesis of pyrimidine and quinolone conjugates as a scaffold for dual inhibitors of HIV reverse transcriptase and integrase

Zhengqiang Wang, Robert Vince

Center for Drug Design

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

44 Scopus citations

Abstract

A series of conjugates combining a pyrimidine and a quinolone moiety were designed and synthesized. The assay results show that these compounds demonstrate both anti-RT activity and anti-IN activity and therefore provide a useful scaffold for identifying inhibitors with balanced dual activities.

Original language	English (US)
Pages (from-to)	1293-1296
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	18
Issue number	4
DOIs	https://doi.org/10.1016/j.bmcl.2008.01.025
State	Published - Feb 15 2008

Bibliographical note

Funding Information:
This research was supported by the Center for Drug Design at the University of Minnesota. We thank Dr. Eric Bennett for discussion, Dr. Christine Salomon for IN assay, and Christine Dreis for RT assay. We also thank Roger Ptak at Southern Research Institute for cell-based assay and Dr. Robert Craigie of NIH for the integrase plasmid.

Copyright:
Copyright 2008 Elsevier B.V., All rights reserved.

Keywords

Dual inhibitor
HIV
Integrase
Rational design
Reverse transcriptase

UN SDGs

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

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10.1016/j.bmcl.2008.01.025

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title = "Synthesis of pyrimidine and quinolone conjugates as a scaffold for dual inhibitors of HIV reverse transcriptase and integrase",

abstract = "A series of conjugates combining a pyrimidine and a quinolone moiety were designed and synthesized. The assay results show that these compounds demonstrate both anti-RT activity and anti-IN activity and therefore provide a useful scaffold for identifying inhibitors with balanced dual activities.",

keywords = "Dual inhibitor, HIV, Integrase, Rational design, Reverse transcriptase",

author = "Zhengqiang Wang and Robert Vince",

note = "Funding Information: This research was supported by the Center for Drug Design at the University of Minnesota. We thank Dr. Eric Bennett for discussion, Dr. Christine Salomon for IN assay, and Christine Dreis for RT assay. We also thank Roger Ptak at Southern Research Institute for cell-based assay and Dr. Robert Craigie of NIH for the integrase plasmid. Copyright: Copyright 2008 Elsevier B.V., All rights reserved.",

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AU - Vince, Robert

N1 - Funding Information: This research was supported by the Center for Drug Design at the University of Minnesota. We thank Dr. Eric Bennett for discussion, Dr. Christine Salomon for IN assay, and Christine Dreis for RT assay. We also thank Roger Ptak at Southern Research Institute for cell-based assay and Dr. Robert Craigie of NIH for the integrase plasmid. Copyright: Copyright 2008 Elsevier B.V., All rights reserved.

PY - 2008/2/15

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N2 - A series of conjugates combining a pyrimidine and a quinolone moiety were designed and synthesized. The assay results show that these compounds demonstrate both anti-RT activity and anti-IN activity and therefore provide a useful scaffold for identifying inhibitors with balanced dual activities.

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KW - Integrase

KW - Rational design

KW - Reverse transcriptase

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JO - Bioorganic and Medicinal Chemistry Letters

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ER -

Synthesis of pyrimidine and quinolone conjugates as a scaffold for dual inhibitors of HIV reverse transcriptase and integrase

Abstract

Bibliographical note

Keywords

UN SDGs

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