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19 Results Found

  • Article
  • Open Access
7 Citations
4,093 Views
15 Pages

1-(3-chlorophenyl)piperazine (mCPP) is a wide spread new psychoactive substance produces stimulant and hallucinogenic effects similar to those sought from ecstasy. Hence, in the recent years, mCPP has been introduced by the organized crime through th...

(This article belongs to the Special Issue Chromogenic and Fluorogenic Chemosensors)
  • Short Note
  • Open Access
173 Views
7 Pages

20 October 2026

A new hybrid heterocyclic compound, 2-[(4-amino-4H-1,2,4-triazol-3-yl)sulfanyl]-1-[4-(4-chlorophenyl)piperazin-1-yl]ethan-1-one (3), was synthesized by the reaction of 4-amino-4H-1,2,4-triazole-3-thione with 2-chloro-1-[4-(4-chlorophenyl)piperazin-1-...

  • Short Note
  • Open Access
1 Citations
2,989 Views
2 Pages

1 August 2005

In continuation of our interest on synthesis and properties of arylpiperazine derivatives investigated as a serotonin receptors ligands [1,2,3], herein we presented one-pot synthesis of N-{(2Z)-4-[4-(3-chlorophenyl)piperazin-1-yl]but-2-enyl}-1,8-naph...

  • Short Note
  • Open Access
1 Citations
1,463 Views
7 Pages

2 December 2025

Heterocyclic systems such as 1,2,4-triazoles and piperazines play an important role in modern medicinal chemistry due to their structural diversity and broad spectrum of biological activities. In this Short Note, we report the synthesis and spectrosc...

  • Short Note
  • Open Access
2 Citations
6,518 Views
5 Pages

12 January 2023

The novel compound 2-{[4-(4-bromophenyl)piperazin-1-yl)]methyl}-4-(3-chlorophenyl-5-(4-methoxyphenyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione is obtained in good yield via a three-step protocol. The product’s structure is assigned by HRMS, IR, 1...

(This article belongs to the Section Organic Synthesis and Biosynthesis)
  • Article
  • Open Access
9 Citations
3,672 Views
17 Pages

New Piperazine Derivatives of 6-Acetyl-7-hydroxy-4-methylcoumarin as 5-HT1A Receptor Agents

  • Kinga Ostrowska,
  • Anna Leśniak,
  • Weronika Gryczka,
  • Łukasz Dobrzycki and ,
  • Magdalena Bujalska-Zadrożny and
  • Bartosz Trzaskowski
  • + 1 author+ 0 author

1 February 2023

A series of 15 new derivatives of 6-acetyl-7-hydroxy-4-methylcoumarin containing a piperazine group were designed with the help of computational methods and were synthesized to study their affinity for the serotonin 5-HT1A and 5-HT2A receptors. Among...

(This article belongs to the Section Molecular Pharmacology)
  • Article
  • Open Access
4 Citations
3,921 Views
15 Pages

New, Eco-Friendly Method for Synthesis of 3-Chlorophenyl and 1,1′-Biphenyl Piperazinylhexyl Trazodone Analogues with Dual 5-HT1A/5-HT7 Affinity and Its Antidepressant-like Activity

  • Przemysław Zaręba,
  • Anna Partyka,
  • Gniewomir Latacz,
  • Grzegorz Satała and ,
  • Paweł Zajdel and
  • Jolanta Jaśkowska
  • + 1 author+ 0 author

26 October 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)-...

(This article belongs to the Special Issue Current Approaches of Medicinal Chemistry in Neurological and Psychiatric Diseases)
  • Article
  • Open Access
26 Citations
8,509 Views
19 Pages

Microwave-Assisted Synthesis of Trazodone and Its Derivatives as New 5-HT1A Ligands: Binding and Docking Studies

  • Jolanta Jaśkowska,
  • Przemysław Zaręba,
  • Paweł Śliwa,
  • Edyta Pindelska and ,
  • Grzegorz Satała and
  • Zbigniew Majka
  • + 1 author+ 0 author

23 April 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. Our research aimed to develop a new method for the sy...

(This article belongs to the Special Issue Sustainable Synthesis)
  • Article
  • Open Access
7 Citations
3,188 Views
15 Pages

Ultrasound-Assisted Synthesis and In Silico Modeling of Methanesulfonyl-Piperazine-Based Dithiocarbamates as Potential Anticancer, Thrombolytic, and Hemolytic Structural Motifs

  • Freeha Hafeez,
  • Ameer Fawad Zahoor,
  • Azhar Rasul,
  • Asim Mansha and ,
  • Razia Noreen,
  • Zohaib Raza,
  • Kulsoom Ghulam Ali,
  • Ali Irfan and
  • Gamal A. El-Hiti
  • + 4 authors+ 0 author

26 July 2022

Piperazine-based dithiocarbamates serve as important scaffolds for numerous pharmacologically active drugs. The current study investigates the design and synthesis of a series of dithiocarbamates with a piperazine unit as well as their biological act...

(This article belongs to the Special Issue In Silico Methods Applied in Drug and Pesticide Discovery)
  • Article
  • Open Access
104 Citations
13,761 Views
12 Pages

Synthesis and Antimicrobial Activities of Some New 1,2,4-Triazole Derivatives

  • Hakan Bektaş,
  • Nesrin Karaali,
  • Deniz Şahin,
  • Ahmet Demirbaş and ,
  • Şengül Alpay Karaoglu and
  • Neslihan Demirbaş
  • + 1 author+ 0 author

8 April 2010

Some novel 4,5-disubstituted-2,4-dihydro-3H-1,2,4-triazol-3-one (3, 6, 8, 9) derivatives and or 3-(4-methylphenyl)[1,2,4]triazolo[3,4-b][1,3]benzoxazole (5) were synthesized from the reaction of various ester ethoxycarbonylhydrazones (1a-e) with seve...

  • Article
  • Open Access
20 Citations
6,017 Views
16 Pages

Synthesis, Anticonvulsant, and Antinociceptive Activity of New 3-(2-Chlorophenyl)- and 3-(3-Chlorophenyl)-2,5-dioxo-pyrrolidin-1-yl-acetamides

  • Małgorzata Góra,
  • Anna Czopek,
  • Anna Rapacz,
  • Anna Gębska and ,
  • Katarzyna Wójcik-Pszczoła,
  • Elżbieta Pękala and
  • Krzysztof Kamiński
  • + 2 authors+ 0 author

12 March 2021

The new series of 3-(2-chlorophenyl)- and 3-(3-chlorophenyl)-pyrrolidine-2,5-dione-acetamide derivatives as potential anticonvulsant and analgesic agents was synthesized. The compounds obtained were evaluated in the following acute models of epilepsy...

(This article belongs to the Special Issue Design and Development of New Compounds/Strategies for the Neuropathic Pain Management)
  • Article
  • Open Access
18 Citations
7,860 Views
16 Pages

1 July 2015

A series of novel 4-substituted-N-(phenylcarbamoyl)-3-pyridinesulfonamides 11–27 have been synthesized by the reaction of 4-substituted pyridine-3-sulfonamides 2–10 with the appropriate aryl isocyanates in presence of potassium carbonate. The in vitr...

(This article belongs to the Collection Efficient Pharmaceutical and Chemical Approaches for Anticancer Therapy: Design, Preliminary Evaluations, and Further Developments)
  • Article
  • Open Access
27 Citations
5,983 Views
14 Pages

Synthesis and Antimicrobial Activity of New Mannich Bases with Piperazine Moiety

  • Sara Janowska,
  • Sylwia Andrzejczuk,
  • Piotr Gawryś and
  • Monika Wujec

21 July 2023

A series of novel Mannich bases were designed, synthesized, and screened for their antimicrobial activity. The target compounds were synthesized from 4-(3-chlorophenyl)-5-(3-fluorophenyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione and different piperazin...

(This article belongs to the Special Issue Novel Antibacterial Agents: Discovery, Design, Synthesis, and Evaluation)
  • Article
  • Open Access
34 Citations
10,248 Views
14 Pages

Synthesis and Cytotoxic Activity of Some Novel N-Pyridinyl-2-(6-phenylimidazo[2,1-b]thiazol-3-yl)acetamide Derivatives

  • Huaiwei Ding,
  • Zhe Chen,
  • Cunlong Zhang,
  • Tian Xin and ,
  • Yini Wang,
  • Hongrui Song,
  • Yuyang Jiang,
  • Yuzong Chen,
  • Yongnan Xu and
  • Chunyan Tan
  • + 5 authors+ 0 author

23 April 2012

A series of novel compounds bearing imidazo[2,1-b]thiazole scaffolds were designed and synthesized based on the optimization of the virtual screening hit compound N-(6-morpholinopyridin-3-yl)-2-(6-phenylimidazo[2,1-b]thiazol-3-yl)acetamide (5a), and...

(This article belongs to the Section Medicinal Chemistry)
  • Article
  • Open Access
13 Citations
4,415 Views
22 Pages

New 5-Aryl-1,3,4-Thiadiazole-Based Anticancer Agents: Design, Synthesis, In Vitro Biological Evaluation and In Vivo Radioactive Tracing Studies

  • Rana M. El-Masry,
  • Basma M. Essa,
  • Adli A. Selim,
  • Soad Z. El-Emam and ,
  • Khaled O. Mohamed,
  • Tamer M. Sakr,
  • Hanan H. Kadry,
  • Azza T. Taher and
  • Sahar M. Abou-Seri
  • + 4 authors+ 0 author

27 November 2022

A new series of 5-(4-chlorophenyl)-1,3,4-thiadiazole-based compounds featuring pyridinium (3), substituted piperazines (4a–g), benzyl piperidine (4i), and aryl aminothiazoles (5a–e) heterocycles were synthesized. Evaluation of the cytotox...

(This article belongs to the Section Medicinal Chemistry)
  • Article
  • Open Access
1 Citations
2,171 Views
13 Pages

A Novel Compound from the Phenylsulfonylpiperazine Class: Evaluation of In Vitro Activity on Luminal Breast Cancer Cells

  • Fernanda Cardoso da Silva,
  • Ana Clara Cassiano Martinho,
  • Helen Soares Valença Ferreira,
  • Raoni Pais Siqueira and ,
  • Vinicius Marques Arruda,
  • Joyce Ferreira da Costa Guerra,
  • Maria Laura dos Reis de Souza,
  • Emanuelly Silva Landin,
  • Celso de Oliveira Rezende Júnior and
  • Thaise Gonçalves de Araújo
  • + 5 authors+ 0 author

20 September 2024

Breast cancer (BC) is the most common cancer in women, and is characterized by its histological and molecular heterogeneity. Luminal BC is an estrogen receptor-positive subtype, with varied clinical courses. Although BC patients are eligible for horm...

(This article belongs to the Special Issue Heterocycles: Design, Synthesis and Biological Evaluation, 2nd Edition)
  • Systematic Review
  • Open Access
29 Citations
21,123 Views
46 Pages

Pharmacological Treatments for Cocaine Craving: What Is the Way Forward? A Systematic Review

  • Dângela Layne Silva Lassi,
  • André Malbergier,
  • André Brooking Negrão,
  • Lígia Florio and ,
  • João P. De Aquino and
  • João Maurício Castaldelli-Maia
  • + 1 author+ 0 author

14 November 2022

Background: cocaine craving is a core feature of cocaine use disorder and remains a critical challenge for abstinence and relapse prevention. This review summarizes the anti-craving efficacy of pharmacotherapies tested for cocaine use disorder, in th...

(This article belongs to the Section Neuropharmacology and Neuropathology)