pyrimidinones and benzofuran

pyrimidinones has been researched along with benzofuran* in 2 studies

Other Studies

2 other study(ies) available for pyrimidinones and benzofuran

Article	Year
Identification of benzofurano[3,2-d]pyrimidin-2-ones, a new series of HIV-1 nucleotide-competing reverse transcriptase inhibitors. Bioorganic & medicinal chemistry letters, 2013, May-01, Volume: 23, Issue:9 Screening of our sample collection led to the identification of a set of benzofurano[3,2-d]pyrimidine-2-one hits acting as nucleotide-competing HIV-1 reverse transcriptase inhibitiors (NcRTI). Significant improvement in antiviral potency was achieved when substituents were introduced at positions N1, C4, C7 and C8 on the benzofuranopyrimidone scaffold. The series was optimized from low micromolar enzymatic activity against HIV-1 RT and no antiviral activity to low nanomolar antiviral potency. Further profiling of inhibitor 30 showed promising overall in vitro properties and also demonstrated that its potency was maintained against viruses resistant to the other major classes of HIV-1 RT inhibitors. Topics: Animals; Benzofurans; HIV Reverse Transcriptase; HIV-1; Humans; Microsomes, Liver; Nucleotides; Protein Binding; Pyrimidinones; Rats; Reverse Transcriptase Inhibitors; Structure-Activity Relationship	2013
Nucleotide competing reverse transcriptase inhibitors: discovery of a series of non-basic benzofurano[3,2-d]pyrimidin-2-one derived inhibitors. Bioorganic & medicinal chemistry letters, 2013, May-01, Volume: 23, Issue:9 A HTS screen led to the identification of a benzofurano[3,2-d]pyrimidin-2-one core structure which upon further optimization resulted in 1 as a potent HIV-1 nucleotide competing reverse transcriptase inhibitor (NcRTI). Investigation of the SAR at N-1 allowed significant improvements in potency and when combined with the incorporation of heterocycles at C-8 resulted in potent analogues not requiring a basic amine to achieve antiviral activity. Additional modifications at N-1 resulted in 33 which demonstrated excellent antiviral potency and improved physicochemical properties. Topics: Benzofurans; Caco-2 Cells; Cell Membrane Permeability; HIV Reverse Transcriptase; HIV-1; Humans; Microsomes, Liver; Nucleotides; Protein Binding; Pyrimidinones; Reverse Transcriptase Inhibitors; Stereoisomerism; Structure-Activity Relationship	2013

Article

Year

Identification of benzofurano[3,2-d]pyrimidin-2-ones, a new series of HIV-1 nucleotide-competing reverse transcriptase inhibitors.

Bioorganic & medicinal chemistry letters, 2013, May-01, Volume: 23, Issue:9

Screening of our sample collection led to the identification of a set of benzofurano[3,2-d]pyrimidine-2-one hits acting as nucleotide-competing HIV-1 reverse transcriptase inhibitiors (NcRTI). Significant improvement in antiviral potency was achieved when substituents were introduced at positions N1, C4, C7 and C8 on the benzofuranopyrimidone scaffold. The series was optimized from low micromolar enzymatic activity against HIV-1 RT and no antiviral activity to low nanomolar antiviral potency. Further profiling of inhibitor 30 showed promising overall in vitro properties and also demonstrated that its potency was maintained against viruses resistant to the other major classes of HIV-1 RT inhibitors.

Topics: Animals; Benzofurans; HIV Reverse Transcriptase; HIV-1; Humans; Microsomes, Liver; Nucleotides; Protein Binding; Pyrimidinones; Rats; Reverse Transcriptase Inhibitors; Structure-Activity Relationship

2013

Nucleotide competing reverse transcriptase inhibitors: discovery of a series of non-basic benzofurano[3,2-d]pyrimidin-2-one derived inhibitors.

Bioorganic & medicinal chemistry letters, 2013, May-01, Volume: 23, Issue:9

A HTS screen led to the identification of a benzofurano[3,2-d]pyrimidin-2-one core structure which upon further optimization resulted in 1 as a potent HIV-1 nucleotide competing reverse transcriptase inhibitor (NcRTI). Investigation of the SAR at N-1 allowed significant improvements in potency and when combined with the incorporation of heterocycles at C-8 resulted in potent analogues not requiring a basic amine to achieve antiviral activity. Additional modifications at N-1 resulted in 33 which demonstrated excellent antiviral potency and improved physicochemical properties.

Topics: Benzofurans; Caco-2 Cells; Cell Membrane Permeability; HIV Reverse Transcriptase; HIV-1; Humans; Microsomes, Liver; Nucleotides; Protein Binding; Pyrimidinones; Reverse Transcriptase Inhibitors; Stereoisomerism; Structure-Activity Relationship

2013