Synthesis, evaluation and structure-activity relationships of triazine dimers as novel antiviral agents

M. Venkatraj; K.K. Ariën; J. Heeres; J. Joossens; J. Messagie; J. Michiels; P. Van der Veken; G. Vanham; P.J. Lewi; K. Augustyns

doi:10.1016/j.bmcl.2012.09.066

Synthesis, evaluation and structure-activity relationships of triazine dimers as novel antiviral agents

M. Venkatraj, K.K. Ariën, J. Heeres, J. Joossens, J. Messagie, J. Michiels, P. Van der Veken, G. Vanham, P.J. Lewi, K. Augustyns

Virology

Research output: Contribution to journal › A1: Web of Science-article › peer-review

Abstract

This letter reports the synthesis and structure-activity relationship (SAR) study of a series of triazine dimers as novel antiviral agents. These compounds were obtained through a bivalent ligand approach in which two triazine moieties are covalently connected by suitable linkers. Several compounds showed submicromolar activity against wild-type HIV-1 and moderate activity against single mutant strains.

Original language	English
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	22
Issue number	23
Pages (from-to)	7174-7178
Number of pages	5
ISSN	0960-894X
DOIs	https://doi.org/10.1016/j.bmcl.2012.09.066
Publication status	Published - 2012

Keywords

Viral diseases
HIV-1
AIDS
Microbicides
Development
Antiviral agents
Triazines
Evaluation
Cytotoxicity
Reverse transcriptase
Strains

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10.1016/j.bmcl.2012.09.066

http://www.ncbi.nlm.nih.gov/pubmed/23084903

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title = "Synthesis, evaluation and structure-activity relationships of triazine dimers as novel antiviral agents",

abstract = "This letter reports the synthesis and structure-activity relationship (SAR) study of a series of triazine dimers as novel antiviral agents. These compounds were obtained through a bivalent ligand approach in which two triazine moieties are covalently connected by suitable linkers. Several compounds showed submicromolar activity against wild-type HIV-1 and moderate activity against single mutant strains.",

keywords = "Viral diseases, HIV-1, AIDS, Microbicides, Development, Antiviral agents, Triazines, Evaluation, Cytotoxicity, Reverse transcriptase, Strains",

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TY - JOUR

T1 - Synthesis, evaluation and structure-activity relationships of triazine dimers as novel antiviral agents

AU - Venkatraj, M.

AU - Ariën, K.K.

AU - Heeres, J.

AU - Joossens, J.

AU - Messagie, J.

AU - Michiels, J.

AU - Van der Veken, P.

AU - Vanham, G.

AU - Lewi, P.J.

AU - Augustyns, K.

N1 - ITG-B2A; ITG-B6B; ITG-B8A; DBM; U-VIROL; JIF; DOI; PDF; Abstract; DSPACE

PY - 2012

Y1 - 2012

N2 - This letter reports the synthesis and structure-activity relationship (SAR) study of a series of triazine dimers as novel antiviral agents. These compounds were obtained through a bivalent ligand approach in which two triazine moieties are covalently connected by suitable linkers. Several compounds showed submicromolar activity against wild-type HIV-1 and moderate activity against single mutant strains.

AB - This letter reports the synthesis and structure-activity relationship (SAR) study of a series of triazine dimers as novel antiviral agents. These compounds were obtained through a bivalent ligand approach in which two triazine moieties are covalently connected by suitable linkers. Several compounds showed submicromolar activity against wild-type HIV-1 and moderate activity against single mutant strains.

KW - Viral diseases

KW - HIV-1

KW - AIDS

KW - Microbicides

KW - Development

KW - Antiviral agents

KW - Triazines

KW - Evaluation

KW - Cytotoxicity

KW - Reverse transcriptase

KW - Strains

U2 - 10.1016/j.bmcl.2012.09.066

DO - 10.1016/j.bmcl.2012.09.066

M3 - A1: Web of Science-article

C2 - 23084903

SN - 0960-894X

VL - 22

SP - 7174

EP - 7178

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 23

ER -

Synthesis, evaluation and structure-activity relationships of triazine dimers as novel antiviral agents

Abstract

Keywords

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