280762-20-1Relevant academic research and scientific papers
Aminopropyl-substituted tropane amine compound and its pharmaceutical composition, preparation method and use
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Paragraph 0158; 0192; 0193; 0194; 0195, (2017/08/29)
The invention belongs to the field of pharmaceutical chemistry and discloses a 8-(3-aminopropyl)-3-exo-8-azabicyclo[3. 2. 1]octane-3-amino-amide compound and its pharmaceutical composition and use. The compound or pharmacologically acceptable salt can be
Discovery of bioavailable 4,4-disubstituted piperidines as potent ligands of the chemokine receptor 5 and inhibitors of the human immunodeficiency virus-1
Kazmierski, Wieslaw M.,Aquino, Christopher,Chauder, Brian A.,Deanda, Felix,Ferris, Robert,Jones-Hertzog, Deborah K.,Kenakin, Terrence,Koble, Cecilia S.,Watson, Christian,Wheelan, Pat,Yang, Hanbiao,Youngman, Michael
experimental part, p. 6538 - 6546 (2009/11/30)
We describe robust chemical approaches toward putative CCR5 scaffolds designed in our laboratories. Evaluation of analogues in the 125I-[MIP-1β] binding and Ba-L-HOS antiviral assays resulted in the discovery of 64 and 68 in the 4,4-disubstitited piperidine class H, both potent CCR5 ligands (pIC50 = 8.30 and 9.00, respectively) and HIV-1 inhibitors (pIC50 = 7.80 and 7.84, respectively, in Ba-L-HOS assay). In addition, 64 and 68 were bioavailable in rodents, establishing them as lead molecules for further optimization toward CCR5 clinical candidates.
