Design, synthesis, and pharmacological effects of structurally simple ligands for MT1 and MT2 melatonin receptors
摘要:
A series of phenoxyalkyl and phenylthioalkyl amides were prepared as melatoninergic ligands. Modulation of affinity of the newly synthesized compound by applying SARs around the terminal amide moiety, the alkyl chain, and the methoxy group on the aromatic ring provides compounds with nanomolar affinity for both melatonin receptor subtypes. Affinity towards MT1 and MT2 receptors were modulated also exploiting chirality. The investigation of intrinsic activity revealed that all the tested compounds behave as full or partial agonists. (C) 2010 Elsevier Ltd. All rights reserved.
Design, synthesis, and pharmacological effects of structurally simple ligands for MT1 and MT2 melatonin receptors
摘要:
A series of phenoxyalkyl and phenylthioalkyl amides were prepared as melatoninergic ligands. Modulation of affinity of the newly synthesized compound by applying SARs around the terminal amide moiety, the alkyl chain, and the methoxy group on the aromatic ring provides compounds with nanomolar affinity for both melatonin receptor subtypes. Affinity towards MT1 and MT2 receptors were modulated also exploiting chirality. The investigation of intrinsic activity revealed that all the tested compounds behave as full or partial agonists. (C) 2010 Elsevier Ltd. All rights reserved.
[EN] FUNGICIDAL 4-SUBSTITUTED-3-{PHENYL[(HETEROCYCLYLMETHOXY)IMINO]METHYL}-1,2,4-OXADIZOL-5(4H)-ONE DERIVATIVES<br/>[FR] DÉRIVÉS DE 3-{PHÉNYL[(HÉTÉROCYCLYLMÉTHOXY)IMINO]MÉTHYL}-1,2,4-OXADIZOL-5(4H)-ONE 4-SUBSTITUÉE FONGICIDES
申请人:BAYER IP GMBH
公开号:WO2013037717A1
公开(公告)日:2013-03-21
The present invention provides fungicidal 4-substituted-3-phenyl[(heterocyclylmethoxy)imino]methyl}-1,2,4-oxadiazol-5(4H)-one derivatives of formula (I) wherein A represents a pyridyl or thiazole group and X1, Y1 to Y5 represent independently different substituents.
The present invention provides fungicidal 4-substituted-3-phenyl[(heterocyclylmethoxy)imino]methyl}-1,2,4-oxadiazol-5(4H)-one derivatives of formula (I)
wherein A represents a pyridyl or thiazole group and X1, Y1 to Y5 represent independently different substituents.
A series of phenoxyalkyl and phenylthioalkyl amides were prepared as melatoninergic ligands. Modulation of affinity of the newly synthesized compound by applying SARs around the terminal amide moiety, the alkyl chain, and the methoxy group on the aromatic ring provides compounds with nanomolar affinity for both melatonin receptor subtypes. Affinity towards MT1 and MT2 receptors were modulated also exploiting chirality. The investigation of intrinsic activity revealed that all the tested compounds behave as full or partial agonists. (C) 2010 Elsevier Ltd. All rights reserved.