Results 11 to 20 of about 1,055 (154)

Novel 4,5-Dihydrothiazole-Phenylpiperazine Derivatives: Synthesis, Docking Studies and Pharmacological Evaluation as Serotonergic Agents. [PDF]

ChemMedChem
The synthesis of a new series of 4,5‐dihydrothiazol‐2‐ylphenylpiperazine derivatives as serotoninergic ligands is described and tested for their affinity toward 5‐HT1A, 5‐HT2A,and 5‐HT2C and selected for further in vivo assays to determine their functional activity. The pharmacological studies highlight that among the developed derivatives, FG‐7 and FG‐
Andreozzi G, Karkoszka N, Sparaco R, Corvino A, Severino B, Santagada V, Magli E, Gibuła-Tarłowska E, Kotlińska JH, Gawel K, Capasso R, Lesniak A, Semenko N, Kaczor AA, Bielenica A, Biała G, Caliendo G, Kędzierska E, Fiorino F.   +18 more
europepmc   +2 more sources

Piperazine Derivatives: A Privileged Scaffold in Modern Synthesis and Medicinal Chemistry. [PDF]

ChemistryOpen
Piperazine‐based bioactive molecules represent a versatile class of compounds with broad therapeutic potential. Structural modification of the piperazine scaffold governs key structure–activity relationships, enabling antibacterial, antifungal, antitumor, neuroactive, and anti‐inflammatory activities.
Ten A, Koizhaiganova R, Bissenbay D, Tursynova B, Zhaxibayeva Z, Yu V.   +5 more
europepmc   +2 more sources

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 ...
Mastromarino M, Niso M, Abate C, Proschak E, Dubiel M, Stark H, Castro M, Lacivita E, Leopoldo M.   +8 more
europepmc   +3 more sources

Protective mechanism of arylpiperazine dopaminergic D2ligands on nitric oxide and 6-hydroxydopamine induced SH-SY5Y human neuroblastoma cell death

, 2012
U ovom radu je ispitivan uticaj 20 novosintetisanih arilpiperazinskih dopaminergičkih liganada na vijabilnost humanih SH-SY5Y neuroblastomskih ćelija tretiranih donorom azot monoksida (engl. nitric oxide, NO) natrijum nitroprusidom (engl.
Tovilović, Gordana I.
core   +4 more sources

p38 mitogen‐activated protein kinase: Functions and targeted therapy in diseases

MedComm – Oncology, Volume 2, Issue 3, September 2023., 2023
Our review provides an overview of the relationship between P38 mitogen‐activated protein kinase (p38MAPK) and disease, especially on small‐molecule inhibitors of four p38MAPK subtypes, and summarizes the challenges about the development of p38MAPK inhibitors.
Qinwen Zheng, Shutong Li, Aoxue Wang, Man Zhe, Panpan Yang, Yongya Wu, Min Zhao, Yumeng Zhu, Yi Luo, Guan Wang, Liang Ouyang   +10 more
wiley   +1 more source

Modeling interactions of α1a adrenergic receptor and different arylpiperazine ligands

, 2012
Molecular modelling studies were undertaken in order to identify key interactions of selected ligands with α1A adrenergic receptor, responsible for their binding and presumably receptor activation. The previously made model of α1A adrenergic receptor was
Senćanski, Milan V., Andrić, Deana, Kostić Rajačić, Slađana, Šukalović, Vladimir, Došen-Mićović, Ljiljana, Šoškić, Vukić, Roglić, Goran   +6 more
core   +6 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

Neuroprotective arylpiperazine dopaminergic/serotonergic ligands suppress experimental autoimmune encephalomyelitis in rats [PDF]

, 2015
Arylpiperazine-based dopaminergic/serotonergic ligands exert neuroprotective activity. We examined the effect of arylpiperazine D-2/5-HT1A ligands, N-{4-[2-(4-phenyl-piperazin-1-yl)-ethyl}-phenyl]- picolinamide (6a) and N-{3-[2-(4-phenyl-piperazin-1-yl ...
Trajković, Vladimir, Vladimir Bumbasirevic, Jelena Tosic, Darko Ciric, Stanojević, Željka, Kaveh Shakib, Vukic Soskic, Vladimir Trajkovic, Kostić Rajačić, Slađana, Tosic, Jelena, Isaković, Aleksandra, Kravić-Stevović, Tamara, Martinović, Tamara, Petricevic, Sasa, Šoškić, Vukić, Sasa Petricevic, Ciric, Darko, Zeljka Stanojevic, Verica Paunovic, Paunović, Verica, Bumbasirevic, Vladimir, Marjan Popovic, Tamara Martinovic, Tamara Kravic‐Stevovic, Sladjana Kostic‐Rajacic, Shakib, Kaveh, Popović, Marjan, Aleksandra Isakovic   +27 more
core   +1 more source