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1.
Biomedicines ; 10(2)2022 Feb 05.
Artigo em Inglês | MEDLINE | ID: mdl-35203593

RESUMO

The antimicrobial multidrug resistance (AMR) of pathogenic bacteria towards currently used antibiotics has a remarkable impact on the quality and prolongation of human lives. An effective strategy to fight AMR is the method PhotoDynamic Therapy (PDT). PDT is based on a joint action of a photosensitizer, oxygen, and light within a specific spectrum. This results in the generation of singlet oxygen and other reactive oxygen species that can inactivate the pathogenic cells without further regrowth. This study presents the efficacy of a new Pd(II)- versus Zn(II)-phthalocyanine complexes with peripheral positions of methylpyridiloxy substitution groups (pPdPc and ZnPcMe) towards Gram-negative bacteria Aeromonas hydrophila (A.hydrophila). Zn(II)-phthalocyanine, ZnPcMe was used as a reference compound for in vitro studies, bacause it is well-known with a high photodynamic inactivation ability for different pathogenic microorganisms. The studied new isolates of A.hydrophila were antibiotic-resistant (R) and sensitive (S) strains. The photoinactivation results showed a full effect with 8 µM pPdPc for S strain and with 5 µM ZnPcMe for both R and S strains. Comparison between both new isolates of A.hydrophila (S and R) suggests that the uptakes and more likely photoinactivation efficacy of the applied phthalocyanines are independent of the drug sensitivity of the studied strains.

2.
Molecules ; 26(12)2021 Jun 09.
Artigo em Inglês | MEDLINE | ID: mdl-34207756

RESUMO

Since December 2019, humanity has faced an important global threat. Many studies have been published on the origin, structure, and mechanism of action of the SARS-CoV-2 virus and the treatment of its disease. The priority of scientists all over the world has been to direct their time to research this subject. In this review, we highlight chemical studies and therapeutic approaches to overcome COVID-19 with seven different sections. These sections are the structure and mechanism of action of SARS-CoV-2, immunotherapy and vaccine, computer-aided drug design, repurposing therapeutics for COVID-19, synthesis of new molecular structures against COVID-19, food safety/security and functional food components, and potential natural products against COVID-19. In this work, we aimed to screen all the newly synthesized compounds, repurposing chemicals covering antiviral, anti-inflammatory, antibacterial, antiparasitic, anticancer, antipsychotic, and antihistamine compounds against COVID-19. We also highlight computer-aided approaches to develop an anti-COVID-19 molecule. We explain that some phytochemicals and dietary supplements have been identified as antiviral bioproducts, which have almost been successfully tested against COVID-19. In addition, we present immunotherapy types, targets, immunotherapy and inflammation/mutations of the virus, immune response, and vaccine issues.


Assuntos
COVID-19/prevenção & controle , Antivirais/química , Antivirais/uso terapêutico , Produtos Biológicos/uso terapêutico , COVID-19/patologia , COVID-19/terapia , COVID-19/virologia , Vacinas contra COVID-19/administração & dosagem , Vacinas contra COVID-19/imunologia , Síndrome da Liberação de Citocina/prevenção & controle , Desenho de Fármacos , Reposicionamento de Medicamentos , Humanos , Imunoterapia , SARS-CoV-2/genética , SARS-CoV-2/isolamento & purificação , SARS-CoV-2/fisiologia
3.
MethodsX ; 7: 100896, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32405465

RESUMO

2 nm gold nanoparticles (AuNPs) have promising applications within drug and protein delivery, bioimaging, and biosensing. By performing ligand place-exchange reactions, AuNPs protected with alkanethiolate ligands can be functionalized to regulate their behaviors. In this reaction, a new ligand is incorporated by mixing a thiol with the AuNPs. To remove the excess new ligand as well as the displaced thiolate, dialysis has previously been the most widely used method. However, this purification method is time-consuming and fails to remove unwanted thiols completely. In this study, we describe a fast and efficient procedure to purify AuNP aqueous solution through liquid-liquid extraction using dichloromethane.•We demonstrate a facile way to purify AuNPs after ligand place-exchange reactions through liquid-liquid extraction.•Liquid-liquid extraction is a simple, inexpensive and efficient method for AuNP purification.•This protocol enables us to completely purify AuNPs in a few hours and can be used as a much quicker and more scaleable valid alternative to dialysis.

4.
Mini Rev Med Chem ; 15(9): 789-96, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25723464

RESUMO

Nowadays, heterocyclic compounds which have a nitrogen atom on the structure, such as pharmacological products, pesticides and antimicrobials can be demonstrated by biologically-active groups that serve the pharmaceutical industry and they are still important in this field. Various cyclization reactions form the basis of the literature on the syntheses of heterocyclic compounds. NArylpiperazines are a class of heterocyclic compounds that play an important role in organic synthesis and are generally found as fragments in receptor ligands and natural products. They have been used extensively as reactive species for building chemical diversity. Arylpiperazines are also found in many pharmacologically-active molecules. Our research group has published numerous papers over the last two years on the synthesis of potentially bioactive tandospirone analogues which have a piperazine group by reductive Heck reactions. We also reported some important isoxazoline derivatives by 1,3-dipolar cycloadditions. Our work continued with potentially pharmacologically-active tandospirone analogues which have an exo-ring in the tricyclic system with an oxygen bridge and containing a 3-(trifluoromethyl)phenyl and 2,3-dichlorophenyl group on the aromatic ring.


Assuntos
Antidepressivos/química , Isoindóis/química , Piperazinas/química , Pirimidinas/química , Antidepressivos/síntese química , Antidepressivos/uso terapêutico , Compostos Bicíclicos com Pontes/química , Catálise , Ciclização , Reação de Cicloadição , Transtorno Depressivo/tratamento farmacológico , Humanos , Isoindóis/síntese química , Isoindóis/uso terapêutico , Isoxazóis/química , Espectroscopia de Ressonância Magnética , Paládio/química , Piperazinas/síntese química , Piperazinas/uso terapêutico , Pirimidinas/síntese química , Pirimidinas/uso terapêutico , Espectroscopia de Infravermelho com Transformada de Fourier , Estereoisomerismo
5.
Acta Chim Slov ; 60(1): 87-94, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-23841336

RESUMO

The C-C coupling of N,N'-bis(5-norbornene-2,3-dicarboximide) (3) and N,N'-bis(7-oxa-5-norbornene-2,3-dicarboximide) (6) with aryl and heteroaryl iodides gave under reductive Heck conditions the C-aryl(hetaryl), substituted N,N'-bistricyclic imides 7a-f and 8a,b. The fused spiro-1,3-indandionolylpyrrolidine compounds, 9, 10 and 11 were also obtained from ninhydrine, sarcosine and 3 or 6 via [3+2]cycloaddition.

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