Results 31 to 40 of about 1,089 (172)

Investigation of key interactions between the second extracellular loop of dopamine D2 receptor and several hydroxy-N-{[2-(4-phenyl-piperaziny-1-yl)ethyl]phenyl}-nicotinamides [PDF]

Journal of the Serbian Chemical Society, 2014
Dopaminergic receptor system has been in focus for the development of new pharmacotherapeutic agents, targeting number of central nervous system related disorders, like drug addiction, schizophrenia, depression, and Parkinson's disease, just to ...
Šukalović Vladimir, Šoškić Vukić, Ignjatović Đurđica, Andrić Deana, Penјišević Jelena, Kostić-Rajačić Slađana   +5 more
doaj   +1 more source

New, Eco-Friendly Method for Synthesis of 3-Chlorophenyl and 1,1′-Biphenyl Piperazinylhexyl Trazodone Analogues with Dual 5-HT_1A/5-HT₇ Affinity and Its Antidepressant-like Activity

Molecules, 2022
Serotonin 5-HT1A and 5-HT7 receptors play an important role in the pathogenesis and pharmacotherapy of depression. Previously identified N-hexyl trazodone derivatives, 2-(6-(4-(3-chlorophenyl)piperazin-1-yl)hexyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one ...
Przemysław Zaręba, Anna Partyka, Gniewomir Latacz, Grzegorz Satała, Paweł Zajdel, Jolanta Jaśkowska   +5 more
doaj   +1 more source

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

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

Synthesis of I-arylpiperazine-4-thiocarboxamides [PDF]

, 1969
The reaction of 1-arylpiperazine salts with hot aqueous ammonium thiocyanate for a short time affords only the thiocyanate salts. l-Arylpiperazine-4-thiocarboxamides have been obtained by prolonged heating of the aqueous solutions of the thiocyanate ...
Ghate, S. P., Arya, V. P., Venkateswarlu, A., Nagarajan, K.   +3 more
core   +2 more sources

Hit-To-Lead Optimization of a Pyridylpiperazine Class Against Malaria: Pharmacokinetic Profile and In Vivo Efficacy of Optimized Compounds. [PDF]

ChemMedChem
Chemical optimization of a novel pyridylpiperazine class yields two promising antimalarial candidates with an exceptional balance of metabolic stability and solubility. These optimized leads significantly protect mice from cerebral malaria, reducing parasitic load by up to 91.7%.
Oliveira DDDS, Pereira DE, Chelucci RC, Michelan S, Pituba JMF, Andricopulo AD, Ferreira LLG, Silva NM, Júnior COR.   +8 more
europepmc   +2 more sources

Gd-Complexes of New Arylpiperazinyl Conjugates of DTPA-Bis(amides): Synthesis, Characterization and Magnetic Relaxation Properties

Molecules, 2015
Two new DTPA-bis(amide) based ligands conjugated with the arylpiperazinyl moiety were synthesized and subsequently transformed into their corresponding Gd(III) complexes 1 and 2 of the type [Gd(L)H2O]·nH2O.
Abdullah O. Ba-Salem, Nisar Ullah, M. Nasiruzzaman Shaikh, Mohamed Faiz, Zaheer Ul-Haq   +4 more
doaj   +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