Article
Environmental Sciences
Zainab Rabiu, Mohd Amir Asyraf Mohd Hamzah, Rosnani Hasham, Zainul Akmar Zakaria
Summary: Pyroligneous acid obtained from slow pyrolysis of palm kernel shell has high total phenolic content and exhibits antioxidant and anti-inflammatory activities. Certain fractions showed significant inhibition towards COX-2 and 5-LOX enzymes, indicating potential as alternative antioxidant and anti-inflammatory agents.
ENVIRONMENTAL SCIENCE AND POLLUTION RESEARCH
(2021)
Review
Chemistry, Medicinal
Ali Aliabadi, Elham Khanniri, Mohammad Mahboubi-Rabbani, Maryam Bayanati
Summary: Dual cyclooxygenase 2/15-lipoxygenase inhibitors offer a valuable alternative for the treatment of inflammatory diseases and prevention of cancer, with reduced side effects compared to classical NSAIDs and selective COX-2 inhibitors. This review provides an overview of the COX-2 and 15-LOX pathways and discusses various structural families of dual inhibitors, paving the way for the design of potentially-active anticancer agents with balanced dual inhibition of these enzymes.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Immunology
Aline N. Martins, Dionys de Souza Almeida, Iziara F. Florentino, Lorrane K. da Silva Moreira, Larissa C. Turones, Daniel C. Batista, Lucas S. Machado, Boniek G. Vaz, Luciano M. Liao, Gerlon de Almeida Ribeiro Oliveira, Jose Luis Rodrigues Martins, James Oluwagbamigbe Fajemiroye, Ricardo Menegatti, Elson A. Costa, Daiany P. B. da Silva
Summary: Advances have been made in the search for new multi-target modulators to control pain and inflammation. Therefore, compound LQFM202 was synthesized and evaluated for its effects on COX-1, COX-2, and 5-LOX enzymes. The results showed that LQFM202 inhibited these enzymes and had antinociceptive and anti-inflammatory effects in animal models.
INFLAMMOPHARMACOLOGY
(2023)
Review
Chemistry, Medicinal
Sitansu Sekhar Nanda, Dong Kee Yi, Om Prakash Panda, Sridevi Chigurupati, Tapas Kumar Mohapatra, Md Imran Hossain
Summary: Indazole is a nitrogen-containing heterocyclic compound that possesses special biological properties such as antimicrobial, anti-inflammatory, anticancer, anti-HIV, and antihypertensive actions. Its derivatives also show similar activities and may have potential as new drug candidates.
CURRENT TOPICS IN MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Christophe Tratrat, Anthi Petrou, Maria Fesatidou, Michelyne Haroun, Geronikaki Athina, Katharigatta Venugopala, Nagaraja Sreeharsha, Jad Chemali
Summary: Viral infections can range from mild to severe, with some infections like Hepatitis B, Hepatitis C, and HIV being a major public health concern worldwide. The recent COVID-19 pandemic, caused by the coronavirus, has affected millions of people globally, resulting in significant fatalities. Additionally, the rise of drug-resistant strains poses serious health problems, making it crucial for researchers to develop new antiviral agents to combat mutated and novel viruses. This review focuses on the antiviral activity of five-membered heterocyclic compounds, specifically discussing compounds with thiadiazoles, triazoles, oxadiazoles, and thiazoles as structural components.
CURRENT TOPICS IN MEDICINAL CHEMISTRY
(2023)
Article
Pharmacology & Pharmacy
Ahad Amer Alsaiari, Mazen Almehmadi, Mohammad Asif
Summary: We synthesized new thiazole analogs and tested their antibacterial activity against selected bacterial strains using the cup plate method. By refluxing substituted 4-phenyl thiazol-2-amine derivatives with 4-aminobenzene-1-sulfonyl chloride in the presence of pyridine and acetic anhydride, we synthesized 4-amino-N-(4-phenylthi-azol-2-yl)benzene sulfonamide derivatives (2a-f). The structures of these compounds were confirmed through various analysis methods. The results showed that compounds 2d, 2e, and 2f exhibited good activity against Staphylococcus aureus, compound 2b showed good activity against Bacillus subtilis, and compounds 2c, 2e, and 2f showed good activity against Escherichia coli, while compound 2d showed good activity against Klebsiella pneumoniae.
LATIN AMERICAN JOURNAL OF PHARMACY
(2023)
Article
Chemistry, Medicinal
Minakshi A. Meshram, Utkarsha O. Bhise, Priyanka N. Makhal, Venkata Rao Kaki
Summary: Inflammation is a complex pathological process leading to various diseases, with different treatments available but limitations exist. The development of new, effective, and safe anti-inflammatory agents is needed to address the shortcomings of current treatments.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Review
Multidisciplinary Sciences
Nabarun Mukhopadhyay, Ashtabhuja Shukla, Priyanka N. Makhal, Venkata Rao Kaki
Summary: Inflammation is a complex physiological process with various disorders. Inflammatory mediators produced through an arachidonic acid pathway are responsible for long-term inflammatory conditions such as osteoarthritis, rheumatoid arthritis, asthma, cancer, and neurological disorders. NSAIDs, commonly used to treat inflammation by inhibiting COX and 5-LOX enzymes, have limitations and adverse effects. Therefore, the search for novel, effective, and safer anti-inflammatory agents is crucial. This review article discusses the implications of phytochemicals and bioactive fractions in the development of dual COX-LOX inhibitors, highlighting different classes of phytoconstituents that show significant dual COX-LOX inhibition.
Review
Chemistry, Inorganic & Nuclear
Huzaifa Yasir Khan, Sabiha Parveen, Imtiyaz Yousuf, Sartaj Tabassum, Farukh Arjmand
Summary: Metal complexes of non-steroidal anti-inflammatory drugs (NSAIDs) have gained attention in anti-tumor drug therapy. By selecting suitable metal ions and coordination geometries, NSAID-metal conjugates can be fine-tuned for targeted therapies. Metal complexes exhibit intriguing behavior in vivo, interacting with intracellular molecules and targeting cancer cells, thus playing a significant role in cell inhibition processes.
COORDINATION CHEMISTRY REVIEWS
(2022)
Review
Chemistry, Organic
Mohamed A. Salem, Samir Y. Abbas, Marwa A. M. Sh El-Sharief, Abdullah Y. Alzahrani, Mohamed H. Helal, Hamdy Kh Thabet
Summary: A new series of thiazole derivatives was synthesized using 5-(aryldiazo)salicylaldehyde thiosemicarbazones. The antimicrobial activity of these derivatives was evaluated. Different synthetic methods were used to obtain 4-methylthiazole derivatives and thiazolidin-4-one derivatives.
SYNTHETIC COMMUNICATIONS
(2021)
Article
Chemistry, Multidisciplinary
Muhammad Haroon, Mabilly Cox Holanda de Barros Dias, Aline Caroline da Silva Santos, Valeria Rego Alves Pereira, Luiz Alberto Barros Freitas, Rodolfo Bento Balbinot, Vanessa Kaplum, Celso Vataru Nakamura, Luiz Carlos Alves, Fabio Andre Brayner, Ana Cristina Lima Leite, Tashfeen Akhtar
Summary: The synthesis of novel 1,3-thiazoles and 4-thiazolidinones demonstrated promising activity against Leishmania spp. and Trypanosoma cruzi, with compound 1f showing the most potent effect. Additionally, compound 1f induced necrosis and apoptosis in T. cruzi, leading to parasite death. This study provides potential avenues for scaffold optimization in the development of improved and safer drug candidates for neglected tropical diseases.
Article
Biochemistry & Molecular Biology
Mostafa M. M. El-Miligy, Ahmed K. Al-Kubeisi, Saad R. El-Zemity, Rasha A. Nassra, Marwa M. Abu-Serie, Aly A. Hazzaa
Summary: The study aimed to combat CRC by synthesizing and evaluating new thymol - 4-thiazolidinone hybrids as multitarget anticancer agents that could inhibit the key COX-2, 5-LOX and PIM-1 kinase enzymes simultaneously. Compound 5g showed the most promising results, inhibiting three key targets leading to inhibition of human CRC cell proliferation both in vitro and in vivo.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
K. Uma Priya, Ch. Venkataramaiah, N. Y. Sreedhar, C. Naga Raju
Summary: A series of new sulphonamide and carbamate derivatives were synthesized and evaluated for their antimicrobial and anti-inflammatory activities. The compounds showed promising antimicrobial and anti-inflammatory activities, with identified toxicology risks within potential drug candidate limits. Molecular docking, ADMET, and QSAR studies suggested strong correlation between in silico profiles and in vitro/in vivo results, indicating the synthesized derivatives could potentially be promising drug candidates for future developments.
Article
Chemistry, Physical
Andrii Lozynskyi, Ihor Yushyn, Yulia Shepeta, Olexandr Karpenko, Andrzej K. Gzella, Roman Lesyk
Summary: A series of thiopyrano[2,3d]thiazole derivatives were synthesized via Michael reaction of malononitrile and 5arylideneisorhodanine. The structures of the newly synthesized compounds were established using spectral data and single-crystal X-ray diffraction analysis.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Biochemistry & Molecular Biology
Rania H. Abd El-Hameed, Shahenda Mahgoub, Hend M. El-Shanbaky, Mosaad S. Mohamed, Sahar A. Ali
Summary: In this study, novel compounds were synthesized from furanone derivatives and tested for their anti-inflammatory activities against COX enzymes, 15-LOX, and TNF-alpha. The majority of the compounds showed significant to high activities, with three pyridazinone derivatives identified as the most promising anti-inflammatory agents with dual COX-2/15-LOX inhibition activities and high TNF-alpha inhibition activity.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2021)
Article
Plant Sciences
Gunes Ak, Gokhan Zengin, Stefano Dall'Acqua, Irene Ferrarese, Stefania Sut, Jasmina Glannotlijab, Marina Sokovib, Marija Nenadic, Annalisa Chiavaroli, Lucia Recinella, Sheila Leone, Giustino Orlando, Luigi Menghini, Claudio Ferrante
Summary: The genus Scorzonera is important in traditional medicine systems and this study found that extracts from Scorzonera species have protective and antimicrobial effects on the skin. The extracts contain flavonoids, which may contribute to their skin protective effects. Additionally, the extracts showed antibacterial and antifungal properties, particularly against Trichoderma viride.
Article
Chemistry, Applied
Ljubos Usjak, Milica Drobac, Marija Ivanov, Marina Sokovic, Marina T. Milenkovic, Marjan Niketic, Silvana Petrovic
Summary: The composition and antimicrobial activity of essential oils from different parts of cultivated Pastinaca sativa subsp. sativa, as well as its two wild-growing relatives, P. sativa subsp. urens and P. hirsuta, were investigated. The oils showed variations in composition and activity against various microorganisms.
JOURNAL OF ESSENTIAL OIL RESEARCH
(2023)
Article
Biochemistry & Molecular Biology
Maia Merlani, Nanuli Nadaraia, Lela Amiranashvili, Anthi Petrou, Athina Geronikaki, Ana Ciric, Jasmina Glamoclija, Tamara Carevic, Marina Sokovic
Summary: Twelve steroid-based hydrazones were evaluated in silico as antimicrobial agents using the computer program PASS. Experimental evaluation revealed low to moderate antibacterial activity against all tested bacteria, except for B. cereus. The most potent compound was number 11. It exhibited superior activity against MRSA compared to ampicillin and showed good antifungal activity.
Article
Biochemistry & Molecular Biology
Tamires Barlati Vieira da Silva, Maria Ines Dias, Carla Pereira, Filipa Mandim, Marija Ivanov, Marina Sokovic, Isabel C. F. R. Ferreira, Lillian Barros, Flavio Augusto Vicente Seixas, Adelar Bracht, Rosane Marina Peralta
Summary: Kenyan purple tea is a variety of green tea plant exclusive to Kenya, known for its purple color and high content of anthocyanin polyphenols. This study aimed to identify and quantify the major anthocyanin polyphenols in the purple tea leaves and test its ability to inhibit triglyceride absorption. The results showed that the purple tea extract had strong inhibitory effects on pancreatic lipase and triglyceride digestion, suggesting that regular consumption of Kenyan purple tea may be beneficial for obesity control.
Article
Biochemistry & Molecular Biology
Alexis Pereira, Mikel Anibarro-Ortega, Marina Kostic, Antonio Nogueira, Marina Sokovic, Jose Pinela, Lillian Barros
Summary: This study aimed to upcycle quince peel into bioactive extracts (BEs) and fiber concentrates (FCs) by optimizing the multicomponent extraction processes using response surface methodology (RSM). The BEs were analyzed for phenolic compounds, organic acids, and other constituents, while FCs were characterized for their color and dietary fiber content. The validated extraction conditions resulted in high yields of bioactive constituents and FCs, demonstrating in vitro antioxidant and antimicrobial effects.
Article
Infectious Diseases
Vakhtang Barbakadze, Maia Merlani, Lali Gogilashvili, Lela Amiranashvili, Anthi Petrou, Athina Geronikaki, Ana Ciric, Jasmina Glamoclija, Marina Sokovic
Summary: The antimicrobial activities of biopolymers extracted from six plants of Boraginaceae family were studied. Moderate antibacterial activities were observed, with only three plants showing activities against all tested bacteria. On the other hand, better antifungal activity was observed, with the biopolymers from Borago officinalis stems exhibiting the best activities.
Article
Integrative & Complementary Medicine
Juliana Scanavacca, Wanessa de Campos Bortolucci, Ezilda Jacomassi, Irineia Paulina Baretta, Maria Graciela Iecher Faria, Carla Maria Mariano Fernandez, Vele Tesevic, Jasmina Glamoclija, Marina Sokovic, Nelson Barros Colauto, Giani Andrea Linde, Zilda Cristiani Gazim
Summary: This study evaluated the chemical composition and antimicrobial activity of Tetradenia riparia leaf essential oil. The essential oil showed broad antibacterial and antifungal activity, making it a potential alternative for microbial control.
BOLETIN LATINOAMERICANO Y DEL CARIBE DE PLANTAS MEDICINALES Y AROMATICAS
(2023)
Article
Chemistry, Multidisciplinary
A. Petrou, V. Kartsev, A. Geronikaki, J. Glamoclija, A. Ciric, M. Sokovic
Summary: Nine new derivatives of 2-aminothiazole were tested for their antimicrobial activity against bacteria and fungi. The compounds showed potent antibacterial and antifungal effects, with some exceptions. Compound 8 was found to be the most effective antibacterial agent, while compound 1 exhibited the best antifungal activity. Different bacteria and fungi exhibited varying levels of sensitivity towards the tested compounds. Molecular docking studies revealed the potential mechanisms of action for antibacterial and antifungal activities. Furthermore, all compounds displayed excellent druglikeness scores.
SAR AND QSAR IN ENVIRONMENTAL RESEARCH
(2023)
Article
Food Science & Technology
Tatjana Perovic, Jovana Petrovic, Uros Gasic, Marina Kostic, Ana Ciric
Summary: This study evaluates the potential of methanolic extracts of Celtis australis as a source of compounds with antifungal activity. The extracts contain various bioactive constituents including phenolic acids and flavonoids. They showed higher antifungal activity than a commercial fungicide and no toxic effect on human cells in vitro. Therefore, methanolic extracts of C. australis can be a natural alternative to synthetic fungicides in agriculture.
FOOD SCIENCE & NUTRITION
(2023)
Article
Food Science & Technology
Beatriz Nunes Silva, Vasco Cadavez, Cristina Caleja, Eliana Pereira, Ricardo C. Calhelha, Mikel Anibarro-Ortega, Tiane Finimundy, Marina Kostic, Marina Sokovic, Jose Antonio Teixeira, Lillian Barros, Ursula Gonzales-Barron
Summary: This study aimed to characterize the polyphenolic profile and bioactive properties of lemon balm, sage, and spearmint extracts. The results showed that some of these extracts may have the ability to prevent food spoilage and promote health benefits while not displaying toxicity against healthy cells. Although sage extracts did not exhibit anti-inflammatory capacity, they often showed the best outcomes in terms of other bioactivities. Overall, the research provides insight into the potential of plant extracts as a source of active phytochemicals and as natural food additives.
Review
Infectious Diseases
Dejan Stojkovic, Jovana Petrovic, Tamara Carevic, Marina Sokovic, Konstantinos Liaras
Summary: This narrative review provides an overview of the potential of novel synthetic and semisynthetic compounds as antibacterials that target virulence traits in antibiotic-resistant strains. The review focuses on recent research and discusses a range of compounds that show promise in combating antibiotic resistance by targeting bacterial virulence factors. The findings suggest that further research is needed to identify and optimize new compounds with the potential to combat antibiotic-resistant bacterial infections.
Article
Chemistry, Multidisciplinary
Mirjana Peric, Aleksandra Cairovic, Aleksandra Spadijer Gostovic, Dragan Stanimirovic, Marina Kostic, Marija Ivanov, Ana Ciric, Jasmina Glamoclija, Vladimir B. Pavlovic
Summary: This study evaluated the surface texture and biofilm adhesion of veneered or CAD/CAM milled zirconia after professional oral hygiene procedures. The results showed that routine methods of oral hygiene professional maintenance can damage the surfaces of glazed zirconia restorations.
APPLIED SCIENCES-BASEL
(2023)
Article
Horticulture
Angela Fernandes, Nikolaos Polyzos, Filipa Mandim, Carla Pereira, Jovana Petrovic, Marina Sokovic, Spyridon A. Petropoulos
Summary: The aim of this study was to evaluate the effects of different biostimulant formulations with various application regimes, combined with or without mineral fertilizers, on the yield parameters and fruit quality of watermelon plants. The results showed that the W5 treatment resulted in the highest yield due to increased fruit formation. Different treatments had varying effects on the content of fat, proteins, carbohydrates, sugars, and acids in the watermelon fruit.
