887615-87-4Relevant academic research and scientific papers
A Palladium(II)-Catalyzed C-H Activation Cascade Sequence for Polyheterocycle Formation
Cooper, Stephen P.,Booker-Milburn, Kevin I.
, p. 6496 - 6500 (2015/06/02)
Polyheterocycles are found in many natural products and are useful moieties in functional materials and drug design. As part of a program towards the synthesis of Stemona alkaloids, a novel palladium(II)-catalyzed C-H activation strategy for the construction of such systems has been developed. Starting from simple 1,3-dienyl-substituted heterocycles, a large range of polycyclic systems containing pyrrole, indole, furan and thiophene moieties can be synthesized in a single step. Don't overdo it: A palladium(II)-catalyzed C-H activation cascade sequence for the synthesis of polyheterocycles is reported. Aromatization of the initially formed dihydro species occurred with a quinone oxidant. In some cases the use of one equivalent of the oxidant enabled isolation of the dihydro species as a single isomer (see scheme; X=NMe, O, S).
Synthesis and pharmacological evaluation of indole-based sigma receptor ligands
Mésangeau, Christophe,Amata, Emanuele,Alsharif, Walid,Seminerio, Michael J.,Robson, Matthew J.,Matsumoto, Rae R.,Poupaert, Jacques H.,McCurdy, Christopher R.
experimental part, p. 5154 - 5161 (2011/11/29)
A series of novel indole-based analogs were prepared and their affinities for sigma receptors were determined using in vitro radioligand binding assays. The results of this study identified several compounds with nanomolar sigma-2 affinity and significant
Low molecular weight indole fragments as IMPDH inhibitors
Beevers, Rebekah E.,Buckley, George M.,Davies, Natasha,Fraser, Joanne L.,Galvin, Francis C.,Hannah, Duncan R.,Haughan, Alan F.,Jenkins, Kerry,Mack, Stephen R.,Pitt, William R.,Ratcliffe, Andrew J.,Richard, Marianna D.,Sabin, Verity,Sharpe, Andrew,Williams, Sophie C.
, p. 2535 - 2538 (2007/10/03)
The study of non-oxazole containing indole fragments as inhibitors of inosine monophosphate dehydrogenase (IMPDH) is described. The synthesis and in vitro inhibitory values for IMPDH II are discussed.
