Results 21 to 30 of about 310 (140)

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

Design and Synthesis of Arylpiperazine Serotonergic/Dopaminergic Ligands with Neuroprotective Properties [PDF]

Molecules, 2022
Long-chain arylpiperazine scaffold is a versatile template to design central nervous system (CNS) drugs that target serotonin and dopamine receptors. Here we describe the synthesis and biological evaluation of ten new arylpiperazine derivatives designed to obtain an affinity profile at serotonin 5-HT1A, 5-HT2A, 5-HT7 receptor, and dopamine D2 receptor ...
Margherita Mastromarino, Mauro Niso, Carmen Abate, Ewgenij Proschak, Mariam Dubiel, Holger Stark, Marián Castro, Enza Lacivita, Marcello Leopoldo   +8 more
openaire   +4 more sources

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

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

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