Results 31 to 40 of about 310 (140)

Synthesis and Experimental Validation of New Designed Heterocyclic Compounds with Antiproliferative Activity versus Breast Cancer Cell Lines MCF‐7 and MDA‐MB‐231

Journal of Chemistry, Volume 2017, Issue 1, 2017., 2017
Recent drug discovery efforts are highly focused towards identification, design, and synthesis of small molecules as anticancer agents. With this aim, we recently designed and synthesized novel compounds with high efficacy and specificity for the treatment of breast tumors.
Vincenza Barresi, Carmela Bonaccorso, Domenico A. Cristaldi, Maria N. Modica, Nicolò Musso, Valeria Pittalà, Loredana Salerno, Cosimo G. Fortuna, Oliver Sutcliffe   +8 more
wiley   +1 more source

Synthesis of Some New Thiazole Derivatives and Their Biological Activity Evaluation

Journal of Chemistry, Volume 2015, Issue 1, 2015., 2015
New 2‐(4‐arylpiperazine‐1‐yl)‐N‐[4‐(2‐(4‐substituted phenyl)thiazol‐4‐yl)phenyl]acetamide derivatives were synthesized and evaluated for their antimicrobial and anticholinesterase activities. Acetylcholinesterase inhibitory activities of the compounds were found weak contrary to expectations. It is unlikely that antifungal activity of the compounds was
Leyla Yurttaş, Yusuf Özkay, Hülya Karaca Gençer, Ulviye Acar, Filomena Conforti   +4 more
wiley   +1 more source

5‐HT2A receptor agonism by tert‐leucinamide and valinamide synthetic cannabinoids: In vitro and in vivo evidence

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose New synthetic cannabinoid receptor agonists (SCRAs) are associated with severe adverse effects, including unexpected psychiatric symptoms. These compounds are mainly active through their potent agonism on the cannabinoid receptors CB1 and CB2.
Giorgia Corli, Deborah Rudin, Dino Luethi, Matthias E. Liechti, Sabrine Bilel, Matteo Marti, Henrik Green, Manuela Carla Monti, Caitlyn Norman   +8 more
wiley   +1 more source

Ionization constants and partition coefficients of 1-arylpiperazine derivatives

Journal of Pharmacy and Pharmacology, 1985
AbstractThe ionization constant (pKa and liposolubilities (log P) of fourteen 1-arylpiperazines were determined by n-octanol/buffer partition. pKa varied little across the entire series. Log P values ranged from less than 1 to about 2 for the highly lipophilic derivatives of the preset series.
S, Caccia, M H, Fong, R, Urso
openaire   +2 more sources

Piperazine Derivatives: A Privileged Scaffold in Modern Synthesis and Medicinal Chemistry

ChemistryOpen, Volume 15, Issue 1, January 2026.
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.
Assel Ten, Raushan Koizhaiganova, Dilnaz Bissenbay, Bagila Tursynova, Zhanar Zhaxibayeva, Valentina Yu   +5 more
wiley   +1 more source

Recent Advances in Isatin–Thiazole Hybrids: Synthesis, Structural Design, and Biological Application

Chemistry &Biodiversity, Volume 22, Issue 12, December 2025.
ABSTRACT Isatin–thiazole hybrids are considered privileged chemical scaffolds due to their broad spectrum of pharmacological properties, making them attractive candidates for drug development. As a result, isatin–thiazole derivatives have emerged as a prominent class of hybrid heterocycles and have been the focus of extensive research in recent years ...
Isadora M. G. Andrade, Edson de O. Lima Filho, Caio F. Valadão, Luana da S. M. Forezi, Fernando de C. da Silva   +4 more
wiley   +1 more source

Solid-Phase Synthesis of Arylpiperazine Derivatives and Implementation of the Distributed Drug Discovery (D3) Project in the Search for CNS Agents

Molecules, 2011
We have successfully implemented the concept of Distributed Drug Discovery (D3) in the search for CNS agents. Herein, we demonstrate, for the first time, student engagement from different sites around the globe in the development of new biologically ...
William L. Scott, Ziniu Zhou, Martin J. O’Donnell, Grzegorz Satała, Andrzej J. Bojarski, Jean Martinez, Gaël Nomezine, Maciej Pawłowski, Gilles Subra, Katarzyna Grychowska, Joanna Król, Paweł Zajdel   +11 more
doaj   +1 more source

Novel 4,5‐Dihydrothiazole‐Phenylpiperazine Derivatives: Synthesis, Docking Studies and Pharmacological Evaluation as Serotonergic Agents

ChemMedChem, Volume 20, Issue 15, August 2, 2025.
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‐
Giorgia Andreozzi, Natalia Karkoszka, Rosa Sparaco, Angela Corvino, Beatrice Severino, Vincenzo Santagada, Elisa Magli, Ewa Gibuła‐Tarłowska, Jolanta H. Kotlińska, Kinga Gawel, Raffaele Capasso, Anna Lesniak, Nataliia Semenko, Agnieszka A. Kaczor, Anna Bielenica, Grażyna Biała, Giuseppe Caliendo, Ewa Kędzierska, Ferdinando Fiorino   +18 more
wiley   +1 more source

Microwave-Assisted Synthesis of Trazodone and Its Derivatives as New 5-HT_1A Ligands: Binding and Docking Studies

Molecules, 2019
Trazodone, a well-known antidepressant drug widely used throughout the world, works as a 5-hydroxytryptamine (5-HT2) and α1-adrenergic receptor antagonist and a serotonin reuptake inhibitor.
Jolanta Jaśkowska, Przemysław Zaręba, Paweł Śliwa, Edyta Pindelska, Grzegorz Satała, Zbigniew Majka   +5 more
doaj   +1 more source

Towards the convergent therapeutic potential of G protein‐coupled receptors in autism spectrum disorders

British Journal of Pharmacology, Volume 182, Issue 14, Page 3044-3067, July 2025.
Abstract Autism spectrum disorders (ASDs) are diagnosed in 1/100 children worldwide, based on two core symptoms: deficits in social interaction and communication, and stereotyped behaviours. G protein‐coupled receptors (GPCRs) are the largest family of cell‐surface receptors that transduce extracellular signals to convergent intracellular signalling ...
Anil Annamneedi, Caroline Gora, Ana Dudas, Xavier Leray, Véronique Bozon, Pascale Crépieux, Lucie P. Pellissier   +6 more
wiley   +1 more source