A5008781693- Synthesis and Biological Evaluation
- Phenothiazines and Benzothiazines Synthesis and Activities
- Receptor Mechanisms and Signaling
- Neurotransmitter Receptor Influence on Behavior
- Synthesis and Reactions of Organic Compounds
- Pharmacological Receptor Mechanisms and Effects
- Fluorine in Organic Chemistry
- Chemical synthesis and alkaloids
- Chemical Synthesis and Analysis
- Neuroscience and Neuropharmacology Research
- Synthesis and pharmacology of benzodiazepine derivatives
- Quinazolinone synthesis and applications
- Synthesis and Reactivity of Heterocycles
- Cyclopropane Reaction Mechanisms
- Synthesis and bioactivity of alkaloids
- Structural and Chemical Analysis of Organic and Inorganic Compounds
- Coordination Chemistry and Organometallics
- Asymmetric Synthesis and Catalysis
- Analytical Chemistry and Chromatography
- Synthesis and biological activity
- Adenosine and Purinergic Signaling
- Nicotinic Acetylcholine Receptors Study
- Multicomponent Synthesis of Heterocycles
- Organic and Inorganic Chemical Reactions
- Chemical Reaction Mechanisms
Maj Institute of Pharmacology
2008-2024
Polish Academy of Sciences
2011-2024
Medicina
1999-2013
Lukasiewicz Research Network - Krakow Institute of Technology
2000-2013
Georgia State University
2010
Jagiellonian University
1999-2006
Université de Montpellier
2004
Institute of Pharmacology
1995
Abstract magnified image The addition reaction of lithium reagents to the 4 position 2‐chloropyrimidine or 2‐chloroquinazoline followed by oxidation resultant dihydro intermediate product is a powerful tool for synthesis 4‐substituted 2‐chloropyrimidines 2‐chloroquinazolines. 4‐Vinyl derivatives undergo conjugate nucleophilic across vinyl group. A displacement chloride in 2‐chloroquinazolines treatment with 4‐methylpiperazine provides compounds that are antagonists serotonin 5‐HT 2A...
Recent data has indicated that Zn can modulate serotonergic function through the 5-HT1A receptor (5-HT1AR); however, exact mechanisms are unknown. In present studies, radioligand binding assays and behavioural approaches were used to characterize pharmacological profile of at 5-HT1ARs in more detail. The influence on agonist stably expressed HEK293 cells was investigated by vitro methods using [3H]-8-OH-DPAT. vivo effects compared with those 8-OH-DPAT hypothermia, lower lip retraction (LLR),...
Following the glutamatergic theory of schizophrenia and based on our previous study regarding antipsychotic-like activity mGlu7 NAMs, we synthesized a new compound library containing 103 members, which were examined for NAM in T-REx 293 cell line expressing recombinant human receptor. Out twenty-two scaffolds examined, active compounds found only within quinazolinone chemotype. 2-(2-Chlorophenyl)-6-(2,3-dimethoxyphenyl)-3-methylquinazolin-4(3H)-one (A9-7, ALX-171, IC50 = 6.14 µM) was...
Abstract The synthesis and evaluation as 5‐HT 1A 7 serotonin receptor ligands of the two sets O ‐substituted hydroxybenzamides, structurally related to 2‐{3‐[4‐(2‐methoxyphenyl)piperazin‐1‐yl]propoxy}benzamide ( 1 ), K i = 21 nM, 234 nM) are reported. To affect affinity for receptors, an amide moiety 2 , 3 4 5 6 ) a hydrocarbon chain length 8 9 10 were modified. serotonergic activity compounds was generally higher in case receptors compared with ones; most active being meta‐ isomer both...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTStructure-activity relationship studies of central nervous system (CNS) agents. 5. Effect the hydrocarbon chain on affinity 4-substituted 1-(3-chlorophenyl)piperazines for 5-HT1A receptor sitesJerzy L. Mokrosz, Marzena Pietrasiewicz, Beata Duszynska, and Marek T. CeglaCite this: J. Med. Chem. 1992, 35, 13, 2369–2374Publication Date (Print):June 1, 1992Publication History Published online1 May 2002Published inissue 1 June...
Abstract A series of new long‐chain arylpiperazine (LCAP) derivatives with flexible and partly constrained alkyl linker were synthesized investigated in vitro as potential serotonin 5‐HT 1A 7 receptor ligands. The compounds prepared by a two‐step procedure using naphthalimide 2 H‐ 1,3‐benzoxazine‐2,4(3 H )‐dione imides, 1‐(2‐methoxyphenyl)piperazine ( o ‐OMe‐PhP) 1,2,3,4‐tetrahydroisoquinoline (THIQ) amine pharmacophores. Modifications the spacer structure included introduction penta‐...
A new analog of buspirone (1), i.e., 8-[4-[2-(1,2,3,4-tetrahydroisoquinolinyl)]butyl]-8-azaspiro- [4.5]decane-7,9-dione (6a), was synthesized. In demonstrated that and its 6a were equipotent 5-HT(1A) ligands. Several behavioral models showed had essentially the same functional profile at receptors as buspirone. The obtained results permit a conclusion basic nitrogen atom terminal, bulky cycloimide moiety, but not 2-pyrimidinyl group, are directly involved in formation bioactive complex with...
An efficient solid-supported method for the synthesis of a new class arylpiperazine derivatives containing amino acid residues has been developed. A 72-membered library was synthesized on SynPhase Lanterns functionalized by BAL linker. one-pot cleavage/cyclization step aspartic and glutamic yielded succinimide- pyroglutamyl-containing ligands (chemsets 9 10). The representatives under study showed different levels affinity 5-HT1A 5-HT2A receptors (estimated Ki = 24−4000 1−2130 nM,...
The allosteric regulation of G protein-coupled receptors (GPCRs) is a well-known phenomenon, but there are only few examples modulation within the metabotropic serotonergic receptor family. Recently, we described zinc non-competitive interactions toward agonist binding at serotonin 5-HT1A receptors, in which biphasic effects, involving potentiation sub-micromolar concentrations (10 μM) and inhibition sub-millimolar (500 Zn2+ radioligand assays, were consistent with both antagonist-like...
New 1H,3H-pyrimido[2,1-f]purine-2,4-dione derivatives of arylpiperazine (11−22) were prepared and evaluated in vitro for their affinity 5-HT1A, 5-HT2A, α1, D2 receptors. The tested compounds showed high 5-HT1A α1 receptors (Ki = 1.1−87 10−62 nM, respectively) moderate to low 5-HT2A 56−881 nM) 94−1245 nM). Compounds 14, 15, 18, 19, 21, mostly 3'-chlorophenylpiperazine derivatives, can be classified as mixed 5-HT1A/5-HT2A/α1 ligands. Compound 13, which the highest receptor 1.1 nM), was 50-fold...