SAR-studies on the importance of aromatic ring topologies in search for selective 5-HT7 receptor ligands among phenylpiperazine hydantoin derivatives

J Handzlik, AJ Bojarski, G Satała, M Kubacka… - European Journal of …, 2014 - Elsevier
The current study is focused on newly developed phenylpiperazine derivatives of aromatic
methylhydantoin differing in mutual positions of methyl and phenyl moieties. The new …

The multiobjective based design, synthesis and evaluation of the arylsulfonamide/amide derivatives of aryloxyethyl-and arylthioethyl-piperidines and pyrrolidines as a …

P Zajdel, R Kurczab, K Grychowska, G Satała… - European journal of …, 2012 - Elsevier
An analysis of the virtual combinatorial library was used for refining a pilot set of 34
derivatives and designing a targeted 38-member library of the arylamide and …

Discovery of aryl-biphenyl-2-ylmethylpiperazines as novel scaffolds for 5-HT7 ligands and role of the aromatic substituents in binding to the target receptor

Y Kim, J Kim, J Tae, BL Roth, H Rhim, G Keum… - Bioorganic & medicinal …, 2013 - Elsevier
It has been reported that 5-HT7 receptors are promising targets of depression and
neuropathic pain. 5-HT7 receptor antagonists have exhibited antidepressant-like profiles …

Structure−Affinity Relationship Study on N-(1,2,3,4-Tetrahydronaphthalen-1-yl)-4-Aryl-1-Piperazinealkylamides, a New Class of 5-Hydroxytryptamine7 Receptor …

M Leopoldo, F Berardi, NA Colabufo… - Journal of medicinal …, 2004 - ACS Publications
A series of N-(1, 2, 3, 4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides was
prepared and their affinity for serotonin (5-hydroxytryptamine, 5-HT) 5-HT7, 5-HT1A, and 5 …

4-Aminoethylpiperazinyl aryl ketones with 5-HT1A/5-HT7 selectivity

MK Kim, HS Lee, S Kim, SY Cho, BL Roth… - Bioorganic & medicinal …, 2012 - Elsevier
The well-known 5-HT1A/5-HT7 selectivity issue was tackled by a new series of 4-
aminoethylpiperazinyl aryl ketones (1a–1l) specifically designed to distinguish the two …

5-HT7 receptor modulators: Amino groups attached to biphenyl scaffold determine functional activity

Y Kim, H Park, J Lee, J Tae, HJ Kim, SJ Min… - European journal of …, 2016 - Elsevier
HT 7 receptor (5-HT 7 R) agonists and antagonists have been reported to be used for
treatment of neuropathic pain and depression, respectively. In this study, as a novel scaffold …

trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines:  A New Class of Potent and Selective 5-HT1A Receptor Ligands as Conformationally Constrained …

R Perrone, F Berardi, NA Colabufo… - Journal of medicinal …, 2001 - ACS Publications
The present paper concerns the influence of conformational parameters on the recognition
by rat 5-HT1A receptors of derivatives 4-[3-(5-methoxy-1, 2, 3, 4-tetrahydronaphthalen-1-yl) …

Rational design in search for 5-phenylhydantoin selective 5-HT7R antagonists. Molecular modeling, synthesis and biological evaluation

K Kucwaj-Brysz, D Warszycki, S Podlewska… - European journal of …, 2016 - Elsevier
A series of novel arylpiperazine 5-(4-fluorophenyl)-5-methylhydantoins with 2-hydroxypropyl
linker (2–15) was synthesized and evaluated on their affinity towards serotonin 5-HT 7 …

New N-and O-arylpiperazinylalkyl pyrimidines and 2-methylquinazolines derivatives as 5-HT7 and 5-HT1A receptor ligands: synthesis, structure-activity relationships …

S Intagliata, MN Modica, V Pittalà, L Salerno… - Bioorganic & medicinal …, 2017 - Elsevier
Based on our earlier studies of structure activity relationships on 4-substituted piperazine
derivatives, in this work we synthesized a novel set of long-chain arylpiperazines with the …

SB-656104-A: a novel 5-HT7 receptor antagonist with improved in vivo properties

IT Forbes, S Douglas, AD Gribble, RJ Ife… - Bioorganic & medicinal …, 2002 - Elsevier
A focused SAR study around the previously reported selective 5-HT7 receptor antagonist,
SB-269970-A has resulted in the identification of a structurally related analogue having an …