863436-75-3

Upstream product

• 74-89-5 methylamine 

Downstream Products

• 863442-12-0 7-(4-Fluorobenzyl)-4-hydroxy-1-[2-(isopropylamino)-2-oxoethyl]-N-methyl-2-oxo-1,2-dihydro-1,5-naphthyridine-3-carboxamide 
• 863442-13-1 1-(2-{[2-(Dimethylamino)ethyl]amino}-2-oxoethyl)-7-(4-fluorobenzyl)-4-hydroxy-N-methyl-2-oxo-1,2-dihydro-1,5-naphthyridine-3-carboxamide 
• 863442-11-9 7-(4-Fluorobenzyl)-4-hydroxy-N-methyl-2-oxo-1-{2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl}-1,2-dihydro-1,5-naphthyridine-3-carboxamide 
• 863442-20-0 7-(4-Fluorobenzyl)-4-hydroxy-1-{2-[(2-methoxyethyl)amino]-2-oxoethyl}-N-methyl-2-oxo-1,2-dihydro-1,5-naphthyridine-3-carboxamide 
• 863442-17-5 1-{2-[(Cyclopropylmethyl)amino]-2-oxoethyl}-7-(4-fluorobenzyl)-4-hydroxy-N-methyl-2-oxo-1,2-dihydro-1,5-naphthyridine-3-carboxamide 
• 863442-18-6 7-(4-Fluorobenzyl)-4-hydroxy-N-methyl-2-oxo-1-[2-oxo-2-(propylamino)ethyl]-1,2-dihydro-1,5-naphthyridine-3-carboxamide 
• 863442-37-9 1-[2-(tert-Butylamino)-2-oxoethyl]-7-(4-fluorobenzyl)-4-hydroxy-N-methyl-2-oxo-1,2-dihydro-1,5-naphthyridine-3-carboxamide 

Relevant academic research and scientific papers

Naphthyridinone (NTD) integrase inhibitors 4. Investigating N1 acetamide substituent effects with C3 amide groups

A series of N1 acetamide substituted naphthyridinone HIV-1 integrase inhibitors have been explored to understand structure-activity relationships (SAR) with various C3 amide groups. Investigations were evaluated using integrase enzyme inhibition, antiviral activity and protein binding effects to optimize the sub-structures. Lipophilicity was also incorporated to understand ligand lipophilic efficiency as a function of the structural modifications. Three representative analogs were further examined in a peripheral blood mononuclear cell (PBMC) antiviral assay as well as in vitro and in vivo drug metabolism and pharmacokinetic studies.

HIV INTEGRASE INHIBITORS

The present invention features compounds that are HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.

Naphthyridinone (NTD) integrase inhibitors 4. Investigating N1 acetamide substituent effects with C3 amide groups

A series of N1 acetamide substituted naphthyridinone HIV-1 integrase inhibitors have been explored to understand structure-activity relationships (SAR) with various C3 amide groups. Investigations were evaluated using integrase enzyme inhibition, antiviral activity and protein binding effects to optimize the sub-structures. Lipophilicity was also incorporated to understand ligand lipophilic efficiency as a function of the structural modifications. Three representative analogs were further examined in a peripheral blood mononuclear cell (PBMC) antiviral assay as well as in vitro and in vivo drug metabolism and pharmacokinetic studies.