Results 31 to 40 of about 629 (164)

Synthesis and Critical View on the Structure-Activity Relationships of N-(Substituted phenyl)-/N-Diphenylmethyl-piperazine-Based Conjugates as Antimycobacterial Agents

Applied Sciences, 2021
This research focused on a three-step synthesis, analytical, physicochemical, and biological evaluation of hybrid molecules 6a–g, containing a lipophilic 3-trifluoromethylphenyl moiety, polar carbamoyloxy bridge, 2-hydroxypropan-1,3-diyl chain and 4 ...
Jana Čurillová, Mária Pecháčová, Tereza Padrtová, Daniel Pecher, Šárka Mascaretti, Josef Jampílek, Ľudmila Pašková, František Bilka, Gustáv Kováč, Ivan Malík   +9 more
doaj   +1 more source

Investigation of antibacterial activity of cinnamyl derivatives of arylpiperazine [PDF]

Archives of Biological Sciences, 2012
The derivatives of cinnamic acid and N-arylpiperazine show antibacterial activity. In this work the potential synergistic effect of cinnamyl derivatives of arylpiperazine in selected bacteria was investigated. The antibacterial activities of the derivatives were evaluated against Gram-positive bacteria: Staphylococcus aureus ...
Irena Novakovic, Jelena Penjisevic, V. Sukalovic, Deana Andric, G. Roglic, Sladjana Kostic-Rajacic   +5 more
openaire   +3 more sources

Synthesis, computational and pharmacological evaluation of novel N-{4-[2-(4-aryl-piperazin-1-yl)ethyl]phenyl}-arylamides [PDF]

Journal of the Serbian Chemical Society
Serotonin, or 5-hydroxytryptamine (5-HT), is a biogenic amine most noted as a neurotransmitter, an activator of the utmost subtype family of G-protein- coupled receptors (GPCR). Drugs targeting 5-HT1A and other 5-HT receptors treat central nervous system
Andrić Deana B., Dukić-Stefanović Slađana, Krunić Mihajlo J., Jevtić Ivana I., Penjišević Jelena Z., Šukalović Vladimir B., Kostić-Rajačić Slađana   +6 more
doaj   +1 more source

Synthesis, Docking Studies and Biological Evaluation of Benzo[b]thiophen-2-yl-3-(4-arylpiperazin-1-yl)-propan-1-one Derivatives on 5-HT1A Serotonin Receptors

Molecules, 2012
A series of novel benzo[b]thiophen-2-yl-3-(4-arylpiperazin-1-yl)-propan-1-one derivatives 6a–f, 7a–f and their corresponding alcohols 8a–f were synthesized and evaluated for their affinity towards 5-HT1A receptors.
Ramiro Araya-Maturana, Claudio Saitz Barría, Gerald Zapata-Torres, C. David Pessoa-Mahana, Gonzalo Recabarren-Gajardo, Jenny Fiedler Temer, Hernán Pessoa-Mahana   +6 more
doaj   +1 more source

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

Chemistry Central Journal, 2018
A series of azinesulfonamide derivatives of long-chain arylpiperazines with variable-length alkylene spacers between sulfonamide and 4-arylpiperazine moiety is designed, synthesized, and biologically evaluated.
Krzysztof Marciniec, Rafał Kurczab, Maria Książek, Ewa Bębenek, Elwira Chrobak, Grzegorz Satała, Andrzej J. Bojarski, Joachim Kusz, Paweł Zajdel   +8 more
doaj   +1 more source

Synthesis and In Vitro Antimycobacterial Activity of Novel N-Arylpiperazines Containing an Ethane-1,2-diyl Connecting Chain

Molecules, 2017
Novel 1-(2-{3-/4-[(alkoxycarbonyl)amino]phenyl}-2-hydroxyethyl)-4-(2-fluorophenyl)-piperazin-1-ium chlorides (alkoxy = methoxy to butoxy; 8a–h) have been designed and synthesized through multistep reactions as a part of on-going research programme ...
Tomáš Goněc, Ivan Malík, Jozef Csöllei, Josef Jampílek, Jiřina Stolaříková, Ivan Solovič, Peter Mikuš, Stanislava Keltošová, Peter Kollár, Jim O’Mahony, Aidan Coffey   +10 more
doaj   +1 more source

Interaction of Arylpiperazines with the Dopamine Receptor D2 Binding Site [PDF]

Arzneimittelforschung, 2011
The docking of several 1-benzyl-4-arylpiperazines to the dopamine receptor (DAR) D2 was examined. The results demonstrated that the interaction of protonated N1 of the piperazine ring with Asp 86 (III.32) and edge-to-face interactions of the aromatic ring of the arylpiperazine part of the ligand with Phe 178 (VI.44), Trp 182 (VI.48) and Tyr 216 (VII.58)
Šukalović, Vladimir, Zlatović, Mario, Andrić, Deana, Roglić, Goran, Kostić Rajačić, Slađana, Šoškić, Vukić   +5 more
openaire   +4 more sources

A perspective on multi‐target drug discovery and design for complex diseases

Clinical and Translational Medicine, Volume 7, Issue 1, December 2018., 2018
AbstractDiseases of infection, of neurodegeneration (such as Alzheimer's and Parkinson's diseases), and of malignancy (cancers) have complex and varied causative factors. Modern drug discovery has the power to identify potential modulators for multiple targets from millions of compounds.
Rona R. Ramsay, Marija R. Popovic‐Nikolic, Katarina Nikolic, Elisa Uliassi, Maria Laura Bolognesi   +4 more
wiley   +1 more source

A Versatile and Practical Microwave-Assisted Synthesis of Sterically Hindered N-Arylpiperazines

, 2016
A wide-ranging and practical synthesis of structurally diverse, sterically hindered N-arylpiperazines from 2,2′-(4-nitrophenylsulfonylazanediyl) bis(ethane-2,1-diyl) bis(4-nitrobenzenesulfonate) and substituted anilines has been achieved using microwave ...
Rong Gao (476219), Daniel J. Canney (2254384)   +1 more
core   +1 more source

5‐HT2A receptor agonism by tert‐leucinamide and valinamide synthetic cannabinoids: In vitro and in vivo evidence

British Journal of Pharmacology, Volume 183, Issue 16, Page 4715-4734, August 2026.
Abstract Background and Purpose New synthetic cannabinoid receptor agonists (SCRAs) are associated with severe adverse effects, including unexpected psychiatric symptoms. These compounds are mainly active through their potent agonism on the cannabinoid receptors CB1 and CB2.
Giorgia Corli, Deborah Rudin, Dino Luethi, Matthias E. Liechti, Sabrine Bilel, Matteo Marti, Henrik Green, Manuela Carla Monti, Caitlyn Norman   +8 more
wiley   +1 more source