Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs)

M Venkatraj; KK Ariën; J Heeres; B Dirié; J Joossens; S Van Goethem; P Van der Veken; J Michiels; CML Vande Velde; G Vanham; PJ Lewi; K Augustyns

doi:10.1016/j.bmc.2011.08.060

Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs)

M Venkatraj
, KK Ariën
, J Heeres
, B Dirié
, J Joossens
, S Van Goethem
, P Van der Veken
, J Michiels
, CML Vande Velde
, G Vanham
, PJ Lewi
, K Augustyns

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

Abstract

In this Letter, we report on diarylpyridinone, diarylpyridazinone and diarylphthalazinone analogs as potential inhibitors of HIV-1 nonnucleoside reverse transcriptase (NNRTIs). The most promising compounds in these series are three diarylpyridazinones 25a, 25l and 25n which demonstrated submicromolar activity against wild-type HIV-1 and moderate activity against the single mutant strain Ba-L V106A.

Original language	English
Journal	Bioorganic and Medicinal Chemistry
Volume	19
Issue number	20
Pages (from-to)	5924-5934
Number of pages	11
ISSN	0968-0896
DOIs	https://doi.org/10.1016/j.bmc.2011.08.060
Publication status	Published - 2011

Keywords

B780-tropical-medicine
Viral diseases
HIV-1
AIDS
Non-nucleoside
Reverse transcriptase inhibitors
Mutations
Strains
Diarylpyridinones
Diarylpyridazinones
Diarylphtalazinones
Laboratory techniques and procedures

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10.1016/j.bmc.2011.08.060

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Venkatraj, M., Ariën, KK., Heeres, J., Dirié, B., Joossens, J., Van Goethem, S., Van der Veken, P., Michiels, J., Vande Velde, CML., Vanham, G., Lewi, PJ., & Augustyns, K. (2011). Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs). Bioorganic and Medicinal Chemistry, 19(20), 5924-5934. https://doi.org/10.1016/j.bmc.2011.08.060

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title = "Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs)",

abstract = "In this Letter, we report on diarylpyridinone, diarylpyridazinone and diarylphthalazinone analogs as potential inhibitors of HIV-1 nonnucleoside reverse transcriptase (NNRTIs). The most promising compounds in these series are three diarylpyridazinones 25a, 25l and 25n which demonstrated submicromolar activity against wild-type HIV-1 and moderate activity against the single mutant strain Ba-L V106A.",

keywords = "B780-tropical-medicine, Viral diseases, HIV-1, AIDS, Non-nucleoside, Reverse transcriptase inhibitors, Mutations, Strains, Diarylpyridinones, Diarylpyridazinones, Diarylphtalazinones, Laboratory techniques and procedures",

author = "M Venkatraj and KK Ari{\"e}n and J Heeres and B Diri{\'e} and J Joossens and \{Van Goethem\}, S and \{Van der Veken\}, P and J Michiels and \{Vande Velde\}, CML and G Vanham and PJ Lewi and K Augustyns",

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Venkatraj, M, Ariën, KK, Heeres, J, Dirié, B, Joossens, J, Van Goethem, S, Van der Veken, P, Michiels, J, Vande Velde, CML, Vanham, G, Lewi, PJ & Augustyns, K 2011, 'Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs)', Bioorganic and Medicinal Chemistry, vol. 19, no. 20, pp. 5924-5934. https://doi.org/10.1016/j.bmc.2011.08.060

TY - JOUR

T1 - Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs)

AU - Venkatraj, M

AU - Ariën, KK

AU - Heeres, J

AU - Dirié, B

AU - Joossens, J

AU - Van Goethem, S

AU - Van der Veken, P

AU - Michiels, J

AU - Vande Velde, CML

AU - Vanham, G

AU - Lewi, PJ

AU - Augustyns, K

N1 - FTX abonnement

PY - 2011

Y1 - 2011

N2 - In this Letter, we report on diarylpyridinone, diarylpyridazinone and diarylphthalazinone analogs as potential inhibitors of HIV-1 nonnucleoside reverse transcriptase (NNRTIs). The most promising compounds in these series are three diarylpyridazinones 25a, 25l and 25n which demonstrated submicromolar activity against wild-type HIV-1 and moderate activity against the single mutant strain Ba-L V106A.

AB - In this Letter, we report on diarylpyridinone, diarylpyridazinone and diarylphthalazinone analogs as potential inhibitors of HIV-1 nonnucleoside reverse transcriptase (NNRTIs). The most promising compounds in these series are three diarylpyridazinones 25a, 25l and 25n which demonstrated submicromolar activity against wild-type HIV-1 and moderate activity against the single mutant strain Ba-L V106A.

KW - B780-tropical-medicine

KW - Viral diseases

KW - HIV-1

KW - AIDS

KW - Non-nucleoside

KW - Reverse transcriptase inhibitors

KW - Mutations

KW - Strains

KW - Diarylpyridinones

KW - Diarylpyridazinones

KW - Diarylphtalazinones

KW - Laboratory techniques and procedures

UR - https://www.webofscience.com/wos/woscc/full-record/WOS:000295494600001

U2 - 10.1016/j.bmc.2011.08.060

DO - 10.1016/j.bmc.2011.08.060

M3 - A1: Web of Science-article

C2 - 21930388

SN - 0968-0896

VL - 19

SP - 5924

EP - 5934

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 20

ER -

Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs)

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