Low-Basicity 5-HT Receptor Ligands from the Group of Cyclic Arylguanidine Derivatives and Their Antiproliferative Activity Evaluation.

The serotonin 5-HT receptor (5-HTR), expressed almost exclusively in the brain, affects the Cdk5 signaling as well as the mTOR pathway. Due to the association of 5-HTR signaling with pathways involved in cancer progression, we decided to check the usefulness of 5-HTR ligands in the treatment of CNS tumors. For this purpose, a new group of low-base 5-HTR ligands was developed, belonging to arylsulfonamide derivatives of cyclic arylguanidines.

Green synthesis of 1,3,5-triazine derivatives using a sonochemical protocol.

1,3,5-triazine derivatives are useful compounds with potential applications in various branches of chemical industry, including pharmaceutical chemistry, cosmetic chemistry, photochemistry, and organic chemistry. Due to the growing environmental requirements on conducting efficient, economical, and safe syntheses, development of new methods for synthesizing organic compounds is highly desirable. In this publication, we present a protocol for the synthesis of 1,3,5-triazine derivatives using a sonochemical approach.

A new synthetic ultrasound-assisted method for dibenzoepines.

In this study, we have developed a new ultrasonic synthesis method of dibenzoepines using olanzapine and quetiapine, which are well-known drugs for the treatment of schizophrenia and bipolar disorder. The method is based on the -alkylation reaction of the piperazine fragment in tricyclic compounds with methyl iodide or 2-(2-chloroethoxy)ethanol as the alkylating agent, respectively. The synthesis reactions were carried out in an ultrasonic bath with solvents such as acetonitrile or dimethylformamide in the presence of potassium or sodium carbonate or sodium hydroxide and metal-free, ecological phase transfer catalyst at a temperature of 40-50 °C.

New cyclic arylguanidine scaffolds as a platform for development of antimicrobial and antiviral agents.

According to WHO, infectious diseases are still a significant threat to public health. The combine effects of antibiotic resistance, immunopressure, and mutations within the bacterial and viral genomes necessitates the search for new molecules exhibiting antimicrobial and antiviral activities. Such molecules often contain cyclic guanidine moiety.

Eco-friendly synthesis of new olanzapine derivatives and evaluation of their anticancer potential.

New derivatives of the known antipsychotic drug olanzapine have been obtained as potential compounds with anticancer activity in two metabolically different breast cancer cell lines: MCF-7 and triple negative MDA-MB-231. The compounds were obtained under phase transfer catalysis (PTC) in the presence of microwave irradiation (MW) or ultrasound (")))"), evaluating the effect of solvents such as dimethylformamide, water, or choline chloride/urea (natural deep eutectic solvent, NaDES). In the best option, the compounds were obtained within 2 minutes with a yield of 57-86% in MW.

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

Serotonin 5-HT and 5-HT receptors play an important role in the pathogenesis and pharmacotherapy of depression. Previously identified -hexyl trazodone derivatives, 2-(6-(4-(3-chlorophenyl)piperazin-1-yl)hexyl)-[1,2,4]triazolo[4,3-]pyridin-3(2)-one hydrochloride (), with high affinity for 5-HTR and 2-(6-(4-([1,1'-biphenyl]-2-yl)piperazin-1-yl)hexyl)-[1,2,4]triazolo[4,3-]pyridin-3(2)-one hydrochloride (), a dual-acting 5-HT/5-HT receptor ligand, were prepared with a new microwave-assisted method. The protocol for the synthesis of and involved reductive alkylation under a mild reducing agent.

Eco-friendly methods of synthesis and preliminary biological evaluation of sulfonamide derivatives of cyclic arylguanidines.

The chemotype of arylsulfonamide derivatives of cyclic arylguanidines is a source of molecules with valuable biological activities, including antimicrobial and antitumor properties. The methods of the synthesis presented in the literature are characterized with low selectivity and high environmental nuisance. In this publication, we present a developed alternative and earlier undescribed pathway C, for the synthesis of arylsulfonamide derivatives of cyclic arylguanidines (N-(1H-arylimidazol-2-yl)arylsulfonamides and N-(1,4-dihydroquinazolin-2-yl)arylsulfonamides), including reaction between 2-(methylsulfanyl)-benzimidazole or 2-(methylsulfanyl)-3,4-dihydroquinazoline with arylsulfonamides.

New N-aryl-N'-aryl-/(thio)ureido-/sulfamoylamino-derivatives of alkyl/alkylcarbamoyl piperazines: Effect of structural modifications on selectivity over 5-HT receptor.

The 5-HT receptors are an important biological target in the treatment of CNS diseases. Recently, their importance in the context of non-CNS disease entities has also been postulated. In the light of these reports, we designed a new group of urea derivatives of N-aryl-N'-aryl-/(thio)ureido-/sulfamoylamino-derivatives of alkyl/alkylcarbamoyl piperazines as 5-HTR ligands, focusing on increasing receptor selectivity.

New Pharmaceutical Salts of Trazodone.

New pharmaceutically acceptable salts of trazodone (trazodone hydrogen bromide and trazodone 1-hydroxy-2-naphthonic acid) for the treatment of central nervous system disorders are synthesized and described. Although trazodone salts are poorly crystalline, single-crystal X-ray diffraction data for trazodone 1-hydroxy-2-naphthonic acid were collected and analyzed as well as compared to the previously described crystal structure of commercially available trazodone hydrochloride. The powder samples of all new salts were characterized by Fourier transform infrared spectroscopy, X-ray diffraction and C solid-state nuclear magnetic resonance spectroscopy.

Chemical puzzles in the search for new, flexible derivatives of lurasidone as antipsychotic drugs.

In the pharmacotherapy of schizophrenia, there is a lack of effective drugs, and currently used agents cause a large number of side effects. The D, 5-HT, 5-HT receptors are among the most important receptor targets in the treatment of schizophrenia, but antagonism at 5-HT and 5-HT receptors may bring about additional improvement of cognitive functions. However, doubt exists regarding the importance of 5-HTR in the pharmacotherapy.

Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants.

It is now known that many neurotransmitter systems are responsible for diseases of the central nervous system (CNS). One of the most common CNS disease is depression. Considering that in the treatment and the genesis of depression, the most important are the serotonin receptors from 5-HT, 5-HT, 5-HT and 5-HT groups, and dopamine DR this article describes searching for group of new ligands for mentioned receptors.

New dual ligands for the D and 5-HT receptors from the group of 1,8-naphthyl derivatives of LCAP.

More than 300 million people are suffering from depression, one of the civilization diseases in the 21st century. Serotonin 5-HTR and dopamine DR play an important role in the treatment and pathogenesis of depression. Moreover, in recent years, the efficacy of dual 5-HT/D receptors ligands has been demonstrated in the fight against depression.

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

Trazodone, a well-known antidepressant drug widely used throughout the world, works as a 5-hydroxytryptamine (5-HT) and α-adrenergic receptor antagonist and a serotonin reuptake inhibitor. Our research aimed to develop a new method for the synthesis of trazodone and its derivatives. In the known methods of the synthesis of trazodone and its derivatives, organic and toxic solvents are used, and the synthesis time varies from several to several dozen hours.