422550-69-4Relevant academic research and scientific papers
Feedstocks to Pharmacophores: Cu-Catalyzed Oxidative Arylation of Inexpensive Alkylarenes Enabling Direct Access to Diarylalkanes
Vasilopoulos, Aristidis,Zultanski, Susan L.,Stahl, Shannon S.
, p. 7705 - 7708 (2017)
A Cu-catalyzed method has been identified for selective oxidative arylation of benzylic C-H bonds with arylboronic esters. The resulting 1,1-diarylalkanes are accessed directly from inexpensive alkylarenes containing primary and secondary benzylic C-H bonds, such as toluene or ethylbenzene. All catalyst components are commercially available at low cost, and the arylboronic esters are either commercially available or easily accessible from the commercially available boronic acids. The potential utility of these methods in medicinal chemistry applications is highlighted.
Aza-and polyaza-naphthalenly ketones useful as hiv integrase inhibitors
-
Page/Page column 43, (2010/02/10)
Certain aza- and polyaza-naphthalenyl ketones including certain quinolinyl and naphthyridinyl ketones are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment or the delay in the onset of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
Design and synthesis of 8-hydroxy-[1,6]naphthyridines as novel inhibitors of HIV-1 integrase in vitro and in infected cells
Zhuang, Linghang,Wai, John S.,Embrey, Mark W.,Fisher, Thorsten E.,Egbertson, Melissa S.,Payne, Linda S.,Guare Jr., James P.,Vacca, Joseph P.,Hazuda, Daria J.,Felock, Peter J.,Wolfe, Abigail L.,Stillmock, Kara A.,Witmer, Marc V.,Moyer, Gregory,Schleif, William A.,Gabryelski, Lori J.,Leonard, Yvonne M.,Lynch Jr., Joseph J.,Michelson, Stuart R.,Young, Steven D.
, p. 453 - 456 (2007/10/03)
Naphthyridine 7 inhibits the strand transfer of the integration process catalyzed by integrase with an IC50 of 10 nM and inhibits 95% of the spread of HIV-1 infection in cell culture at 0.39 μM. It does not exhibit cytotoxicity in cell culture
