Results 31 to 40 of about 957 (180)

Modeling of the D-2 dopamine receptor arylpiperazine binding site for 1-{2-[5-(1H-benzimidazoIe-2-thione)]ethyl}-4-arylpiperazines

ChemInform, 2004
Docking of several 1-{2-[5-(1H-benzimidazole-2-thione)]ethyl}-4- and 1-benzylarylpiperazines to the D-2 dopamine receptor (DAR) was examined. The binding pocket of the D-2 DAR defined according to Teeter and DuRand [1] was extended using the Insight II ...
Kostić-Rajačić, Slađana, Deana Andrić, Andrić, Deana, Roglić, Goran, Sladjana Kostić‐Rajacčić, Kostić Rajačić, Slađana, Šukalović, Vladimir, Vukić Šoškić, Mario Zlatović, Goran Roglić, Šoškić, Vukić, Zlatović, Mario, Vladimir Šukalović   +12 more
core   +5 more sources

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

X-ray Crystallography, DFT Calculations and Molecular Docking of Indole-Arylpiperazine Derivatives as α1A-Adrenoceptor Antagonists

Molecules, 2015
Indole-arylpiperazine derivatives have exhibited good selectivity for the α1A-adrenoceptor, but the structure-activity-binding mechanism relationship remains unclear.
Wei Xu, Jun-Jun Huang, Bin-Hao Shao, Xing-Jie Xu, Ren-Wang Jiang, Mu Yuan   +5 more
doaj   +2 more sources

Exploring in silico drug design and pharmacokinetics study for identification of potent antidepressant agents [PDF]

Journal of Chemistry Letters, 2020
In furtherance to our previous study, in silico drug design and pharmacokinetics study were employed on some arylpiperazine derivatives as inhibitors of serotonin transporter (SERT) for identification of potential antidepressant agents.
Sabitu Babatunde Olasupo, Adamu Uzairu, Gideon Shallangwa, Sani Uba   +3 more
doaj   +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

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

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