187221-31-4Relevant articles and documents
NOVEL SUBSTITUTED PIPERAZINE AMIDE COMPOUNDS AS INDOLEAMINE 2, 3-DIOXYGENASE (IDO) INHIBITORS
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, (2020/06/19)
Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
Synthesis by microwave irradiation and binding properties of novel 5-HT1A receptor ligands
Caliendo, Giuseppe,Fiorino, Ferdinando,Perissutti, Elisa,Severino, Beatrice,Gessi, Stefania,Cattabriga, Elena,Borea, Pier Andrea,Santagada, Vincenzo
, p. 873 - 886 (2007/10/03)
This work reports the synthesis by microwave irradiation and the binding tests on the 5-HT1A, 5-HT2A and 5-HT2C receptors of new substituted piperazines in order to identify selective ligands for 5-HT1A subtype receptor. Conventional heating and microwave irradiation of the reactions was compared. Synthesis by microwave irradiation gave the desired compounds in better yields than those obtained by conventional heating. The overall times for the syntheses were considerably reduced. Some resulting active compounds (29 and 39) were characterised by a good selectivity profile for the 5-HT1A subtype receptor. The more active compounds were selected and further evaluated for their binding affinities on D1, D2 dopaminergic and α1, α2 adrenergic receptors. The compound with higher affinity and selectivity for the 5-HT1A over all the considered receptors was the 3-{4-[4-(1,2,3,4-tetrahydronaphthyl)-1-piperazinyl]butan}-benzotriazinone (-)29 (5-HT1A Ki=36 nM, other receptors not active).
Synthesis of 1-[ω-[(arylamino)carbonyl]alkyl]-4-(benzocycloalkyl)piperazines
El-Ahmad, Youssef,Maillet, Philippe,Laurent, Elisabeth,Talab, Akram,Tran, Gilles,Ollivier, Roland
, p. 723 - 734 (2007/10/03)
A series of 1-[co-[(arylamino)carbonyl]alkyl]-4-(benzocycloalkyl)-piperazines (1a-v) was prepared either by reacting the precursor 4-[ω-[(arylamino)carbonyl]alkyl]piperazine (2a-j) with 1-chlorobenzocycloalkanes (3a-c) (Procedure A) or by reacting the N-aryl-ω-chloroalkanamides (5a-j) with the 4-(benzocycloalkyl)piperazines (10a-c) (Procedure B). The best yields were obtained using procedure A.