63307-15-3Relevant academic research and scientific papers
Synthesis and anticholinesterase activity of huperzine a analogues containing phenol and catechol replacements for the pyridone ring
Campiani, Giuseppe,Kozikowski, Alan P.,Wang, Shaomeng,Ming, Liu,Nacci, Vito,Saxena, Ashima,Doctor, Bhupendra P.
, p. 1413 - 1418 (1998)
Based upon modeling results obtained using the crystal structure of huperzine A in complex with acetylcholinesterase (AChE), two novel analogues of this potent AChE inhibitor were designed with phenol or catechol rings replacing the pyridone ring. From the modeling studies, the catechol analogue appeared capable of replacing one of the crystallographic waters bridging huperzine with Tyr 130 and Glu 199 of AChE. The synthesis of these materials by use of a palladium catalyzed bicycloannulation strategy is detailed together with the results of AChE inhibition assays.
Synthesis and Dopaminergic Activity of 2-Substituted Octahydrobenzoquinolines
Craig, J. Cymerman,Torkelson, Steven M.,Findell, Paul R.,Weiner, Richard I.
, p. 961 - 968 (2007/10/02)
A series of 2-substituted octahydrobenzoquinolines has been synthesized and assayed for dopamine agonist activity.Only the compounds corresponding to the β-rotameric conformation of dopamine showed biphasic activity in competition binding studies with the radioligand spiroperidol.These findings suggest that the congeners possessing the β-rotamer conformation show receptor-binding characteristics that resemble those of the ergolines more closely than do those of the corresponding α-rotamer congeners.
