Results 91 to 100 of about 957 (180)

α1-Adrenoceptor antagonists. 5. Pyridazinone-arylpiperazines. Probing the influence on affinity and selectivity of both ortho-Alkoxy groups at the arylpiperazine moiety and cyclic substituents at the pyridazinone nucleus

, 2003
Our previous work on pyridazinone-arylpiperazine derivatives suggested some structural features that a compound should have to show high affinity and good selectivity for alpha(1) adrenoceptors (AR) with respect to alpha(2)-AR.
Floridi M., MANETTI, FABRIZIO, Strappaghetti G., Betti L., BOTTA, MAURIZIO, TAFI, ANDREA, Giannaccini G.   +6 more
core   +2 more sources

Design, Synthesis and Biological Evaluation of Novel N-Arylpiperazines Containing a 4,5-Dihydrothiazole Ring. [PDF]

Pharmaceuticals (Basel), 2023
Andreozzi G, Ambrosio MR, Magli E, Maneli G, Severino B, Corvino A, Sparaco R, Perissutti E, Frecentese F, Santagada V, Leśniak A, Bujalska-Zadrożny M, Caliendo G, Formisano P, Fiorino F.   +14 more
europepmc   +1 more source

Novel 5-HT₇ Receptor Inverse Agonists. Synthesis and Molecular Modeling of Arylpiperazine- and 1,2,3,4-Tetrahydroisoquinoline-Based Arylsulfonamides

, 2016
A series of arylpiperazine- and 1,2,3,4-tetrahydroisoquinoline-based arylsulfonamides was synthesized and evaluated for their interactions with the constitutively active 5-HT7 receptor.
Cor J. Grol (2704648), Jeffrey S. Sprouse (2449516), Anne W. Schmidt (2025853), Håkan V. Wikström (2649832), Erik S. Vermeulen (2704654), Marjan van Smeden (2704651)   +5 more
core   +1 more source

Synthesis of the NK1 Receptor Antagonist GW597599. Part 2: Development of a Scalable Route to a Key Chirally Pure Arylpiperazine

, 2016
GW597599 1 is a novel NK-1 antagonist currently under investigation for the treatment of CNS disorders and emesis. The initial chemical development synthetic route, derived from the one used by medicinal chemistry, involved several hazardous reagents ...
Stefano Curti (2336983), Angelo Maria Manzo (2374669), Giuseppe Guercio (2265895), Stefano Provera (2259523), Michael Goodyear (2336986), Sergio Bacchi (2250403)   +5 more
core   +1 more source

Molecular Research on Mental Disorders. [PDF]

Int J Mol Sci, 2023
Sowa-Kućma M, Stachowicz K.
europepmc   +1 more source

Imidazoles as Serotonin Receptor Modulators for Treatment of Depression: Structural Insights and Structure-Activity Relationship Studies. [PDF]

Pharmaceutics, 2023
Goel KK, Thapliyal S, Kharb R, Joshi G, Negi A, Kumar B.   +5 more
europepmc   +1 more source

Synthesis of the NK1 Receptor Antagonist GW597599. Part 1: Development of a Scalable Route to a Key Chirally Pure Arylpiperazine

, 2016
GW597599 1 is a novel NK-1 antagonist currently under investigation for the treatment of CNS disorders and emesis. The initial synthetic route devised from the medicinal chemistry one, used several hazardous reagents, gave low yields, and produced high ...
Stefano Curti (2336983), Giuseppe Guercio (2265895), Antonella Carangio (2311168), Michael Goodyear (2336986), Sergio Bacchi (2250403), Francesco Tinazzi (2284612)   +5 more
core   +1 more source

The influence of dispersive interactions on the binding affinities of ligands with an arylpiperazine moiety to the dopamine D2 receptor [PDF]

Journal of the Serbian Chemical Society, 2009
Several isosteric 1,3-dihydro-5-[2-(4-aryl-1-piperazinyl)ethyl]-2H-benzimidazole-2-thiones were used to investigate the interactions of different ligands with the binding site of the D2 receptor.
MARIO V. ZLATOVIĆ, VLADIMIR V. ŠUKALOVIĆ, GORAN M. ROGLIĆ, SLAĐANA V. KOSTIĆ-RAJAČIĆ, DEANA B. ANDRIĆ   +4 more
doaj  

Towards metabolically stable 5-HT7 receptor ligands: a study on 1-arylpiperazine derivatives and related isosters

, 2013
Serotonin 7 (5-hydroxytryptamine7 or 5-HT7) is the most recently identified serotonin receptor. It is involved in mood disorders and is studied as a target for antidepressants. Here, we report on the structural manipulation of the 5-HT7 receptor ligand 4-
COLABUFO, Nicola Antonio, LEOPOLDO, Marcello, PERRONE, Roberto, Duszynska B, NISO, MAURO, BERARDI, Francesco, Patarnello D, Bojarski AJ, LACIVITA, ENZA, De Giorgio P, Satala G   +10 more
core   +1 more source

MOESM1 of Structural determinants influencing halogen bonding: a case study on azinesulfonamide analogs of aripiprazole as 5-HT1A, 5-HT7, and D2 receptor ligands

, 2018
Additional file 1: Figure S1. Histograms of population of different arylpiperazine salts conformations. Figure S2. Low-energy conformation of the studied compounds in aqueous medium. Table S1. Conformation of arylpiperazine derivatives with polymethylene
Maria Książek (5205656), Rafał Kurczab (1312479), Paweł Zajdel (2606617), Elwira Chrobak (5205659), Krzysztof Marciniec (2606629), Ewa Bębenek (5205653), Grzegorz Satała (805228), Joachim Kusz (2243047), Andrzej Bojarski (3761443)   +8 more
core   +1 more source