73094-26-5Relevant academic research and scientific papers
Towards novel 5-HT7 versus 5-HT1A receptor ligands among LCAPs with cyclic amino acid amide fragments: Design, synthesis, and antidepressant properties. Part II
Canale, Vittorio,Kurczab, Rafa?,Partyka, Anna,Sata?a, Grzegorz,Witek, Jagna,Jastrz?bska-Wi?sek, Magdalena,Paw?owski, Maciej,Bojarski, Andrzej J.,Weso?owska, Anna,Zajdel, Pawe?
supporting information, p. 202 - 211 (2015/03/18)
A 26-membered library of novel long-chain arylpiperazines, which contained primary and tertiary amides of cyclic amino acids (proline and 1,2,3,4-tetrahydroisoquinoline-3-carboxamide) in the terminal fragment was synthesized and biologically evaluated for binding affinity for 5-HT7 and 5-HT1A receptors. Docking studies confirmed advantages of Tic-amide over Pro-amide fragment for interaction with 5-HT7 receptors. Selected compounds 32 and 28, which behaved as 5-HT7Rs antagonist and 5-HT1A partial agonist, respectively, produced antidepressant-like effects in the forced swim test in mice after acute treatment in doses of 10 mg/kg (32) and 1.25 mg/kg (28). Compound 32 reduced immobility in a manner similar to the selective 5-HT7 antagonist SB-269970.
One-pot enantioselective synthesis of 3-nitro-2H-chromenes catalyzed by a simple 4-hydroxyprolinamide with 4-nitrophenol as cocatalyst
Yin, Guohui,Zhang, Richeng,Li, Lei,Tian, Jun,Chen, Ligong
, p. 5431 - 5438 (2013/09/02)
The asymmetric domino oxa-Michael-Henry reaction of salicylaldehyde derivatives with trans-β-nitro olefins catalyzed by a readily available trans-4-hydroxy-L-prolinamide with 4-nitrophenol as an effective cocatalyst is presented. The corresponding 3-nitro
Amino acids and peptides. XVI. Synthesis of N-terminal tetrapeptide analogs of fibrin α-chain and their inhibitory effects on fibrinogen/thrombin clotting
Kawasaki,Hirase,Miyano,Tsuji,Iwamoto
, p. 3253 - 3260 (2007/10/02)
N-Terminal tetrapeptide analogs of fibrin α-chain were synthesized by the solution method using a new active ester, the ester of the oxime of p-nitroacetophenone, and by the solid-phase method. Their inhibitory effects on fibrinogen/thrombin clotting were examined. Of the synthetic peptides, amide analogs of Gly-Pro-Arg-Pro exhibited a more potent inhibitory effect.
