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- Volume 23, Issue 4, 2023
Current Topics in Medicinal Chemistry - Volume 23, Issue 4, 2023
Volume 23, Issue 4, 2023
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Hydrogen-producing Photocatalyst at Sunscreen for Athletes in Preventing and Healing Muscle-nerve-skin Injuries
By Pathik SahooPhysical injuries in sports are unavoidable, but they can be mitigated and even treated by using molecular hydrogen, which can be administered via a specially formulated sunscreen. The photocatalysts are a special class of semiconductors that can absorb a specific spectrum of light to promote its electron from the valance band (VB) to the conduction band (CB). This creates positively charged holes at VB and negatively charged electrons at CB in generating photochemical reaction centres. Once a photocatalyst that absorbs a harmful UV band from sunlight and can split water is doped inside a hydrogel will produce hydrogen in the presence of sunlight. If we employ such photocatalyst-doped hydrogel over naked skin, the hydrogel will act as a continuous source of water, which will absorb water from sweet, store it inside the hydrogel matrix and deliver it to the photocatalyst for splitting it further into the hydrogen. As a result, such photocatalyst-doped hydrogel can be used as a sunscreen to protect against sunlight and can use that spectrum of light for producing hydrogen from sweat continuously. Hydrogen can be absorbed through the skin and diffused in the body to heal wound-prone or injured muscles, and nerves. Because hydrogen may travel throughout the body, the catalyst-doped hydrogel can be used as a topical gel to treat various ailments such as muscle-nerve skin injuries, cancer, Parkinson's disease, and others. Besides common people, even athletes can use it as sunscreen during sports, which is not feasible for other hydrogen administrating systems.
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Chloroquinolone Carboxamide Derivatives as New Anti-HSV-1 Promising Drugs
Authors: Mariana Souza, Camilly P. P. de Melo, Letícia V. Faro, Luciane Fragel-Madeira, Viveca Giongo, Paula Alvarez Abreu, Fernanda da Costa Santos Boechat, David de Oliveira Silva, Nathalia Motta de Carvalho Tolentino, Claudio Cesar Cirne-Santos, Caroline de Souza Barros, Helena Carla Castro, Marcos Costa de Souza, Maria Cecília Bastos Vieira de Souza and Izabel Christina Nunes de Palmer PaixãoBackground: Since the emergence of HSV resistant strains, new antiviral agents have emerged and still are urgently needed, especially those with alternative targets. Objective: In this work, we evaluated new quinolone derivatives as anti-HSV. Methods: For this study, cells were infected and treated with different components to evaluate the profile of HSV replication in vitro. In addition, studies were performed to determine the pharmacokinetic toxicity and profile of the compound. Results: Indeed the EC50 values of these promising molecules ranged between 8 μM and 32 μM. We have also showed that all compounds inhibited the expression of ICP27 viral proteins, which gives new insights in the search for new target for antiherpetic therapy. Chlorine in positions C6 and phosphonate in position C1 have shown to be important for viral inhibition. The chloroquinolone carboxamide derivatives fulfilled “Lipinsky Rule of Five” for good oral bioavailability and showed higher intestinal absorption and blood brain barrier penetration, as well as lower toxicity profile. Conclusion: Although the inhibition activities of chloroquinolone carboxamide derivatives were lower than acyclovir, they showed different modes of action in comparison to the drugs currently available. These findings encourage us to continue pre-clinical studies for the development of new anti-HSV-1 agents.
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Synthesis, ADMET Prediction, and Antitumor Profile of Phenoxyhydrazine- 1,3-thiazoles Derivatives
Authors: Lucianna Rabelo Pessoa de Siqueira, Larissa Pelágia de Lima Ferreira, Gevanio B. de Oliveira Filho, Marcos Victor Gregório de Oliveira, Aline Ferreira Pinto, Vanessa Gouveia de Melo Silva, Paulo André Teixeira de Moraes Gomes, Marcos Veríssimo de Oliveira Cardoso, Maria de Nazaré Correia Soeiro, Flaviana Alves dos Santos, Maíra Galdino da Rocha Pitta, Janine Siqueira Nunes, Moacyr J. B. de Melo Rego and Ana Cristina Lima LeiteBackground: Cancer is one of the most important barriers to increasing life expectancy in all countries in the 21st century. Investigations of new anti-cancer drugs with low side effects are an urgent demand for medicinal chemists. Considering the known antitumor and immunomodulatory activity of thiazoles, this work presents the synthesis and antineoplastic activity of new thiazoles. Methods: The 22 new compounds (2a-v) were synthesized from different thiosemicarbazones and 2-bromoacetophenone. The compounds were evaluated on: MOLT-4, HL-60, HL-60/MX1, MM1S, SKMEL-28, DU145, MCF-7, and T47d. Results: Compound 2b induced cellular viability on MOLT-4 (37.1%), DU145 (41.5%), and HL- 60/MX1 (58.8%) cells. On MOLT-4 cells, compound 2b exhibited an IC50 of 8.03 μM, and against DU145 cells, an IC50 of 6.04μM. Besides, at IC50 and fold of IC50, 20% to 30% of dead cells were found, most due to necrosis/late apoptosis. Most compounds no showed cytotoxicity against fibroblast cells L929 at the concentrations tested. The compound did not alter the cell cycle of DU145 cells when compared to the negative control. Therefore, compound 2b stands out against DU145 and MOLT-4 cells. Conclusion: Our study reinforced the importance of 1,3-thiazoles nuclei in antitumor activity. In addition, derivative 2b stands out against DU145 and MOLT-4 cells and could be a starting point for developing new antineoplastic agents.
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Nanostructured Transition Metal Sulfide-based Glucose and Lactic Acid Electrochemical Sensors for Clinical Applications
Authors: Mani Arivazhagan, Palanisamy Kannan and Govindhan MaduraiveeranEngineered nanostructures of mixed transition metal sulfides have emerged as promising nanomaterials (NMs) for various electrochemical sensors and biosensors applications, including glucose sensors (GS) and lactic acid sensors (LAS) in clinical aspects. Electrochemical sensors based on nanostructured materials, such as transition metal sulfides and their nanocomposites, including graphene, carbon nanotubes, molecularly imprinted polymers, and metal-organic frameworks, have emerged as potent tools for the monitoring and quantification of biomolecules. Highly sensitive and selective electrochemical detection systems have generally been established credibly by providing new functional surfaces, miniaturization processes, and different nanostructured materials with exceptional characteristics. This review provides an overview of glucose and lactic acid sensors based on transition metal nanomaterials and their nanocomposites with a detailed discussion about the advantages and challenges. The merits of nanoscale transition metal sulphide-based electrochemical sensors and biosensor systems include cost-effectiveness, ease of miniaturization process, energy- and time-efficient, simple preparation, etc. Moreover, online sensing competence is the dynamic strength for sustained progress of electrochemical detection systems, thus fascinating interdisciplinary research. In particular, we discuss the synthesis, characteristics, electrode construction strategies, and uses in electrochemical sensing of glucose and lactic acid primarily based on our most recent research and other reports. In addition, the challenges and future perspectives of the nanostructured transition metal sulfides-based electrochemical sensing and biosensing systems toward the detection of glucose and lactic acid are described.
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Electrochemical Nanomaterial-based Sensors/Biosensors for Drug Monitoring
Determining the amount of medication used is essential for correctly managing treatment systems. The unauthorized use of drugs and the importance of determining the absorbed and required dose of drugs in target organs are essential factors that justify the design of new drug monitoring systems. Electrochemical sensors and biosensors based on nanomaterials have been developed for drug monitoring in the past few years. The use of nanomaterials to optimize the analyte detection process and facilitate electron transfer in electrochemical processes has enhanced intermolecular interactions and increased diagnostic sensitivity. Considering this review, in the first part, the evaluation of cancer drugs is examined, which can be used to determine the exact dose of the drug required in different stages of cancer. Accurate monitoring of cancer drugs can increase patient life expectancy, reduce side effects, and increase economic savings. In the next section, sensors and biosensors designed for antibiotics are examined. Accurate measurement of antibiotics for determining the effectiveness of the dose in controlling infections and preventing antibiotic resistance is possible with the help of these drug diagnostic platforms. In the next part, the diagnosis of different hormones is considered. Abnormal amounts (low/high) of hormones cause multiple physiological complications and various disabilities. Therefore, accurate determination of hormone levels can effectively treat hormonal changes. In the last section, other drugs, including drugs and analgesics for which the use of electrochemical diagnostic platforms can significantly help drug distribution and social health systems, are also discussed.
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Electrochemical Biosensors for Monitoring of Drug-DNA Interactions
More LessThe binding of the therapeutic agents to the nucleic acids is one of the paramount issues in the drug development area that is studied by various techniques. Electrochemical studies have a big portion in this area due to the fact that they allow designing of novel monitoring systems that have superior properties such as being feasible and sustainable. These electrochemical monitoring tools analyze these interactions in in vitro conditions and give the results precisely and rapidly. In the scope of this manuscript, the electrochemical monitoring platforms developed for the determination of DNA-drug interactions were under the spotlight. The electrode types mostly used for the electrochemical monitoring of drug-DNA interactions were described. The binding mechanisms of the drugs to the DNA structure were explained, and the evaluation strategies of the interactions using electrochemical techniques were stated. Most of the reports of the last 25 years were given, and some of the electrochemical biosensor applications including both voltammetric and impedimetric studies were explained in detail. Furthermore, it is possible to reach nanomaterials/biomaterials-based biosensor platforms for the monitoring of DNA-drug interactions, and these applications were in the scope of this manuscript. The future aspects of these areas were also stated.
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Volumes & issues
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Volume 24 (2024)
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Volume 23 (2023)
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Volume 22 (2022)
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Volume 21 (2021)
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Volume 20 (2020)
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Volume 19 (2019)
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Volume 18 (2018)
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Volume 17 (2017)
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Volume 16 (2016)
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Volume 15 (2015)
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Volume 14 (2014)
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Volume 13 (2013)
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Volume 12 (2012)
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Volume 11 (2011)
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Volume 10 (2010)
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Volume 9 (2009)
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Volume 8 (2008)
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Volume 7 (2007)
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Volume 6 (2006)
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Volume 5 (2005)
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Volume 4 (2004)
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Volume 3 (2003)
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Volume 2 (2002)
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Volume 1 (2001)