Results 21 to 30 of about 629 (164)

Synthesis and pharmacological evaluation of several N-(2-nitrophenyl)piperazine derivatives [PDF]

Journal of the Serbian Chemical Society, 2007
Six newly synthesized heterocyclic (2-nitrophenyl)piperazines, with a specific structure of the heteroaryl group, whichmimics the catechol moiety of dopamine (benzimidazoles and substituted benzimidazoles), were evaluated for their binding affinity to ...
DEANA ANDRIC, GORDANA TOVILOVIC, GORAN ROGLIC, DJURDJICA VASKOVIC, VUKIC SOSKIC, MIRKO TOMIC, SLADJANA KOSTIC-RAJACIC   +6 more
doaj   +3 more sources

Synthesis of novel 2-(piperazino-1-yl-alkyl)-1H-benzimidazole derivates and assessment of their interactions with the D2 dopamine receptor [PDF]

Journal of the Serbian Chemical Society, 2019
A total of 14 novel arylpiperazines were synthesized, and pharmacologically evaluated by measuring their affinities towards the D2 dopamine receptor (DRD2) in a [3H]spiperone competition assay.
Penjišević Jelena Z., Andrić Deana B., Šukalović Vladimir B., Roglić Goran M., Šoškić Vukić, Kostić-Rajačić Slađana V.   +5 more
doaj   +1 more source

Synthesis and biological evaluation of 5-substituted derivatives of benzimidazole [PDF]

Journal of the Serbian Chemical Society, 2014
Series of eight novel 5-substituted derivatives of benzimidazole were synthesized by condensation of corresponding diamine with ethyl-4-[4-(2-chlorophenyl)piperazin-1-yl] butanoate in refluxing 4N hydrochloric acid.
Vasić Vesna P., Penjišević Jelena Z., Novaković Irena T., Šukalović Vladimir V., Andrić Deana B., Kostić-Rajačić Slađana V.   +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

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

Pd-Catalyzed Synthesis of Piperazine Scaffolds Under Aerobic and Solvent-Free Conditions. [PDF]

Org Lett, 2016
A facile Pd-catalyzed methodology providing an efficient synthetic route to biologically relevant arylpiperazines under aerobic conditions is reported.
Reilly SW, Mach RH.
europepmc   +2 more sources

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