Results 21 to 30 of about 605 (157)

Influence of N–1 substituent properties on binding affinities of arylpiperazines to the binding site of 5-HT1A receptor [PDF]

Journal of the Serbian Chemical Society, 2006
Serotonin receptors (5-HTRs), especially the 5-HT1A subtype, have been the subject of intensive research for the past decade, due to their function in human physiology.
MARIO V. ZLATOVIC, GORAN M. ROGLIC, DEANA B. ANDRIC, SLADJANA V. KOSTIC-RAJACIC, VLADIMIR V. SUKALOVIC   +4 more
doaj   +3 more sources

Multifaceted Behavior of 2‐Cyanobenzaldehyde and 2‐Acylbenzonitriles in the Synthesis of Isoindolinones, Phthalides and Related Heterocycles

European Journal of Organic Chemistry, Volume 26, Issue 24, June 21, 2023., 2023
Easy access to several classes of heterocyclic compounds is provided by reacting 2‐cyanobenzaldehyde or 2‐acylbenzonitriles with a range of nucleophiles under mild conditions through divergent cascade reactions in an asymmetric way. Abstract 2‐Cyanobenzaldehye (also called 2‐formylbenzonitrile) and related 2‐acylbenzonitriles belong to a class of ...
Mohammad Sadeq Mousavi, Antonia Di Mola, Antonio Massa   +2 more
wiley   +1 more source

Synthesis and Anti‐Mycobacterium tuberculosis Activity of Imidazo[2,1‐b][1,3]oxazine Derivatives against Multidrug‐Resistant Strains

ChemMedChem, Volume 18, Issue 12, June 15, 2023., 2023
Tackling tuberculosis resistance: A hit optimization campaign was performed to optimize a series of previously identified benzofuroxan derivatives. By switching benzofuroxan with the imidazo[2,1‐b][1,3]oxazine subunit, we discovered a new series of leads with superior activity in inhibiting MDR‐Mtb in vitro and intramacrophage mycobacterial growth ...
Guilherme F. S. Fernandes, Karyn F. Manieri, Andressa F. Bonjorno, Debora L. Campos, Camila M. Ribeiro, Fernanda M. Demarqui, Daniel A. G. Ruiz, Nailton M. Nascimento‐Junior, William A. Denny, Andrew M. Thompson, Fernando R. Pavan, Jean L. Dos Santos   +11 more
wiley   +1 more source

Effective chiral pool synthesis of both enantiomers of the TRPML inhibitor trans‐ML‐SI3

Archiv der Pharmazie, Volume 355, Issue 2, February 2022., 2022
An effective chiral pool synthesis of both enantiomers of the TRPML inhibitor trans‐ML‐SI3 was worked out on two different routes, both starting from enantiomerically pure cis‐2‐aminocyclohexanols. The absolute configuration of the more active enantiomer was elucidated. These chiral pool syntheses provide sufficient amounts of the enantiomerically pure
Katharina Kriegler, Charlotte Leser, Peter Mayer, Franz Bracher   +3 more
wiley   +1 more source

Extended N-Arylsulfonylindoles as 5-HT6 Receptor Antagonists: Design, Synthesis & Biological Evaluation

Molecules, 2016
Based on a known pharmacophore model for 5-HT6 receptor antagonists, a series of novel extended derivatives of the N-arylsulfonyindole scaffold were designed and identified as a new class of 5-HT6 receptor modulators.
Gonzalo Vera, Carlos F. Lagos, Sebastián Almendras, Dan Hebel, Francisco Flores, Gissella Valle-Corvalán, C. David Pessoa-Mahana, Jaime Mella-Raipán, Rodrigo Montecinos, Gonzalo Recabarren-Gajardo   +9 more
doaj   +1 more source

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

Discovery and Preliminary SAR of Arylpiperazines as Novel, Brainpenetrant Antiprion Compounds. [PDF]

ACS Med Chem Lett, 2013
Prion diseases are a group of fatal neurodegenerative disorders that include Creutzfeldt-Jakob disease (CJD) and kuru in humans, BSE in cattle, and scrapie in sheep.
Li Z, Gever J, Rao S, Widjaja K, Prusiner SB, Silber BM.   +5 more
europepmc   +2 more sources