Results 91 to 100 of about 310 (140)

Soluble polymer-supported synthesis of arylpiperazines

Tetrahedron Letters, 1998
Abstract A method for soluble, inexpensive polymer-supported synthesis of piperazine and piperidine libraries on the basis of nucleophilic aryl substitution (S n Ar) and N-acylation is reported. Asymmetric N, N′-disubstituted piperazine and piperidine derivatives, that are potential drug candidates, can be synthesized in quantitative yields and ...
Pi-Chi Pan, Chung-Ming Sun
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Spatial structure in the N-arylpiperazine series

Bulletin of the Academy of Sciences of the USSR Division of Chemical Science, 1987
In the compounds examined, the angle of rotation of the plane of the aromatic ring relative to the unshared electron pair of the nitrogen atom is close to orthogonal, but in the o-fluoro-compound it is smaller.
I. Yu. Strobykina, V. E. Kataev, A. N. Vereshchagin, I. V. Galyametdinova, V. D. Akamsin   +4 more
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Solution phase combinatorial synthesis of arylpiperazines

Tetrahedron Letters, 1997
A solution phase combinatorial synthesis of aryl piperazines 1 and 2 is described based on the S(N)Ar reaction and Schotten-Baumann acylation. The use of excess reagent is allowed and pure arylpiperazines 1 and 2 were obtained by simple acid/base washing.
Luc Neuville, Jieping Zhu
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Bioactive conformation of 1-arylpiperazines at central serotonin receptors

Journal of Medicinal Chemistry, 1985
A number of 1-arylpiperazines have been characterized as direct-acting serotonin agonists. Conformational parameters of this class that may affect receptor recognition and binding have been examined through the analysis of X-ray data and synthesis of rigid analogues.
J R, Huff, S W, King, W S, Saari, J P, Springer, G E, Martin, M, Williams   +5 more
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Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential

Bioorganic & Medicinal Chemistry Letters, 2004
Six active compounds, among previously synthesized and screened arylpiperazines, were selected and evaluated for the binding affinity to rat dopamine, serotonin and alpha(1) receptors. Two compounds with benztriazole group had a 5-HT(2A)/D(2) binding ratio characteristic for atypical neuroleptics (>1, pK(i) values).
Tomić, Mirko, Kundaković, Marija, Butorović, Biljana, Petković, Branka, Andrić, Deana, Roglić, Goran, Ignjatović, Đurđica, Kostić-Rajačić, Slađana   +7 more
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Intraocular Pressure Lowering Effects of Novel Arylpiperazine Derivatives

Journal of Ocular Pharmacology and Therapeutics, 1998
Arylpiperazine derivatives were synthesized and investigated in this study. Two animal models, including an intraocular pressure (IOP) recovery method and an alpha-chymotrypsin-induced glaucoma model, were used to determine the ocular pharmacological effects of the arylpiperazine derivatives.
C H, Chiang, T J, Chang, D W, Lu, A R, Lee   +3 more
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Novel arylpiperazines as selective α1-adrenergic receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2000
A novel series of arylpiperazines has been synthesized and identified as antagonists of alpha1a adrenergic receptor (alpha1a-AR) implicated in benign prostatic hyperplasia. These compounds selectively bind to membrane bound alpha1a-AR with K(i)s as low as 0.66 nM.
X, Li, W V, Murray, L, Jolliffe, V, Pulito   +3 more
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The Interactions of the 5-HT3 Receptor with Arylpiperazine, Tropane, and Quinuclidine Ligands

Current Topics in Medicinal Chemistry, 2002
The serotonin 5-HT(3) receptor subtype is unique among the receptors for this neurotransmitter because it has been demonstrated to be a ligand-gated ion channel capable of mediating rapid intercellular communication. This review covers the authors work performed during more than a decade in the development of 5-HT(3) receptor ligands belonging to the ...
Cappelli, Andrea, Anzini, Maurizio, Vomero, Salvatore, Mennuni, L., Makovec, F., Hamon, M., De Benedetti, P. G., Menziani, M. C.   +7 more
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Arylpiperazine substituted heterocycles as Selective α1a adrenergic antagonists

Bioorganic & Medicinal Chemistry Letters, 2002
Antagonists of the alpha(1)-adrenergic receptors (alpha(1)-ARs) are useful for the treatment of benign prostatic hyperplasia. A series of potent and subtype-selective alpha(1a)-AR antagonists has been synthesized, displaying in vitro binding affinity in the low the nanomolar range.
Haripada, Khatuya, Richard H, Hutchings, Gee-Hong, Kuo, Virginia L, Pulito, Linda K, Jolliffe, Xiaobing, Li, William V, Murray   +6 more
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Modeling of the D₂ Dopamine Receptor Arylpiperazine Binding Site for 1‐{2‐[5‐(1H‐Benzimidazole‐2‐thione)]ethyl}‐4‐arylpiperazines.

ChemInform, 2004
AbstractFor Abstract see ChemInform Abstract in Full Text.
Šukalović, Vladimir, Zlatović, Mario, Andrić, Deana, Roglić, Goran, Kostić Rajačić, Slađana, Šoškić, Vukić   +5 more
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