152534-08-2

Upstream product

• 68219-69-2 6-(1-benzoylamino-ethyl)-4,5-dihydro-2H-pyridazin-3-one 
• 68219-76-1 6-(1-benzoylamino-ethyl)-2H-pyridazin-3-one 
• 152534-40-2 (1'RS)-N-<1-(1,6-dihydro-6-oxo-3-pyridazinyl)ethyl>-8-oxo-8-phenyloctanamide 
• 90175-94-3 N-1-(2,3-dihydro-3-oxopyridazin-6-yl)ethylamine hydrochloride 
• 68219-65-8 5-Benzamido-4-oxohexansaeureethylester 
• 152533-92-1 7-(2-Chloro-5-methyl-imidazo[1,5-b]pyridazin-7-yl)-1-phenyl-heptan-1-one 

Relevant academic research and scientific papers

Synthesis and anti-HIV-1 activity of a series of imidazo[1,5- b]pyridazines

A series of substituted imidazo[1,5-b]pyridazines have been prepared and tested for inhibitory activity against the reverse transcriptase of HIV-1 (RT) and their ability to inhibit the growth of infected MT-4 cells. Crystal data are reported on two compounds, 15c and 33. From the structure-activity relationships developed within this and other series, it is proposed that key features of the interaction with RT include hydrogen-bond acceptor and aromatic π-orbital bonding with the imidazopyridazine nucleus and a benzoyl function separated from the heterocycle by a suitable spacer group. Exceptional activity against the reverse transcriptase of HIV-1 (IC50 = 0.65 nM) was obtained with a 2-imidazolyl-substituted derivative, 7-[2-(1H- imidazol-1-yl)-5-methylimidazo[1,5-b]pyridazin-7-yl]-1-phenyl-1-heptanone (33) which is attributed to additional binding of the imidazole sp2 nitrogen atom. A number of the compounds in this series also inhibit the replication of HIV-1 in vitro in MT-4 and C8166 cells at levels observed with the nucleoside AZT.