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: Peer-reviewed journal articles › 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

Cite this

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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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language = "English",

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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: Peer-reviewed journal articles

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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