1032289-55-6Relevant academic research and scientific papers
Convenient strecker reactions of piperidine derivatives with cyclic ketones under aqueous conditions
Murata, Yoshinori,Satake, Kunio
, p. 1485 - 1490 (2008)
Strecker reactions convenient for the preparation of piperidinyl acetonitrile compounds under aqueous conditions are described. The use of TsOH·H2O is the key to afford the desired products in good and reproducible yield. Copyright Taylor & Francis Group,
Structure-activity relationship studies of pyrrolone antimalarial agents
Murugesan, Dinakaran,Kaiser, Marcel,White, Karen L.,Norval, Suzanne,Riley, Jennifer,Wyatt, Paul G.,Charman, Susan A.,Read, Kevin D.,Yeates, Clive,Gilbert, Ian H.
, p. 1537 - 1544 (2013/09/12)
Previously reported pyrrolones, such as TDR32570, exhibited potential as antimalarial agents; however, while these compounds have potent antimalarial activity, they suffer from poor aqueous solubility and metabolic instability. Here, further structure-activity relationship studies are described that aimed to solve the developability issues associated with this series of compounds. In particular, further modifications to the lead pyrrolone, involving replacement of a phenyl ring with a piperidine and removal of a potentially metabolically labile ester by a scaffold hop, gave rise to derivatives with improved in vitro antimalarial activities against Plasmodium falciparum K1, a chloroquine- and pyrimethamine-resistant parasite strain, with some derivatives exhibiting good selectivity for parasite over mammalian (L6) cells. Three representative compounds were selected for evaluation in a rodent model of malaria infection, and the best compound showed improved ability to decrease parasitaemia and a slight increase in survival.
Novel non-peptide nociceptin/orphanin FQ receptor agonist, 1-[1-(1-Methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl] -1H-benzimidazole: Design, synthesis, and structure-activity relationship of oral receptor occupancy in the brain for orally potent
Hayashi, Shigeo,Hirao, Akiko,Imai, Aki,Nakamura, Hiroshi,Murata, Yoshinori,Ohashi, Katsuyo,Nakata, Eriko
experimental part, p. 610 - 625 (2009/12/29)
An endogenous heptadecapeptide, nociceptin/orphanin FQ (N/OFQ), and a G-protein-coupled receptor, N/OFQ peptide (NOP) receptor [or opioid-receptor-like-1 (ORL1) receptor], have been described in terms of its structure, distribution, and pharmacology. Thus
