73816-11-2Relevant articles and documents
The role of polycyclic frameworks in modulating P2X7 receptor function
Callis, Timothy B.,Reekie, Tristan A.,O'Brien-Brown, James,Wong, Erick C.N.,Werry, Eryn L.,Elias, Nabiha,Jorgensen, William T.,Tsanaktsidis, John,Rendina, Louis M.,Kassiou, Michael
, p. 1207 - 1219 (2017/11/24)
Herein we describe our recent attempts to target the P2X7 receptor for potential treatment of neurological disorders. This work focusses on different polycycles including carborane, adamantane or cubane, joined by either a cyanoguanidine or an amide linker to phenyl or isoquinoline moieties. We have demonstrated the superiority of the adamantyl moiety over other polycycles in terms of synthetic accessibility and biological (cellular) activity. We have also shown that an amide or cyanoguanidine linker can greatly alter the biological activity of compounds. This SAR study provides important insights into the types of functionality required to target the P2X7 receptor.
Microwave assisted Leimgruber-Batcho reaction for the preparation of indoles, azaindoles and pyrroylquinolines
Siu, Jason,Baxendale, Ian R.,Ley, Steven V.
, p. 160 - 167 (2007/10/03)
The development of enhanced conditions for Lewis acid catalysed Leimgruber-Batcho indole synthesis using microwave acceleration is described. This approach has permitted the preparation of a variety of heteroaromatic enamine intermediates in good yield and high purities. Subsequent catalytic hydrogenation reactions, under various conditions including the use of a solid-phase encapsulated catalyst, furnish the corresponding indole derivatives in good yields.
Synthesis of (2S)-2-amino-3-(1H-4-indolyl)propanoic acid, a novel tryptophan analog for structural modification of bioactive peptides
Fauq, Abdul H.,Hong, Feng,Cusack, Bernadette,Tyler, Beth M.,Ping-Pang, Yuan,Richelson, Elliott
, p. 4127 - 4134 (2007/10/03)
A convenient, multigram synthesis of a novel α-amino acid (2S)-2- amino-3-(1H-4-indolyl)propanoic acid (la), is reported. An Fmoc-t-Boc derivative of this novel regioisomer of the natural aromatic amino acid tryptophan could be readily incorporated into b