Dihydrofolate reductase inhibitory potential of 1H-indole-based-meldrum linked 1H-1,2,3-triazoles as new anticancer derivatives: In-vitro and in-silico studies.

In this present work, we describe the syntheses of a new series of 32 1H-indole-based-meldrum linked 1H-1,2,3-triazole derivatives (2-13, 15a-15f, 16a-16f, 17a-17f and 19a, 19b, 20a), which constitute a new class of 1H-1,2,3-triazoles. Compounds 15a-15f, 16a-16f, 17a-17f have been prepared by employing "click" reactions between substituted 1H-indole-based meldrum alkynes (11, 12 and 13) and substituted aromatic azides (14a-14f) in the presence of copper iodide (CuI) and Hünig's base. Then, the synthesis of compounds 19, 20 through decomposition of meldrum moiety.

Recent advances on artificial intelligence-based approaches for food adulteration and fraud detection in the food industry: Challenges and opportunities.

Food adulteration is the deceitful practice of misleading consumers about food to profit from it. The threat to public health and food quality or nutritional valuable make it a major issue. Food origin and adulteration should be considered to safeguard customers against fraud.

Triterpenoids from Frankincense and Boswellia: A focus on their pharmacology and C-NMR assignments.

Here we report for the first time the entire C-NMR spectral assignments of 119 (out of 127) triterpenoids from the oleo-gum resins of the medicinally important genus Boswellia, which includes the culturally highly valuable Frankincense species. The complete C-NMR resonances of these triterpenoids isolated between 1998 and 2024 and their biological activities are presented. C-NMR spectroscopy is a highly powerful tool for the characterization of these bioactive natural products.

Biochemical and computational inhibition of α-glucosidase by novel metronidazole-linked 1-1,2,3-triazole and carboxylate moieties: kinetics and dynamic investigations.

In the current study, metronidazole derivatives containing 1-1,2,3-triazole and carboxylate moieties were evaluated and by computational methods for their anti-diabetic potential to insight into their medicinal use for the management of type II diabetes mellitus. Interestingly all 14 compounds displayed high to significant inhibitory capability against the key carbohydrate's digestive enzyme α-glucosidase with IC values in range of 9.73-56.

Efficient microwave synthesis of flurbiprofen derivatives and their enhancement of efficacy in chronic inflammatory pain models and gastro-protective potential in post-operative model.

Present research was designed to synthesize and characterize the flurbiprofen derivatives and to evaluate their analgesic, anti-inflammatory and gastro-protective activities in post-operative and chronic inflammatory pain models. Flurbiprofen derivatives were produced by using three-step processes involving esterification, hydrazide production, and schiff base, each of which modified a different carboxyl group. All the newly synthesized flurbiprofen derivatives () were characterized by H NMR,C NMR,F NMR and HR-ESI-MS, and the post-operative, inflammatory pain and ulcerogenic activities were determined in well-established animal models.

Meldrum-Based-1-1,2,3-Triazoles as Antidiabetic Agents: Synthesis, α-Glucosidase Inhibition Activity, Molecular Docking Studies, and Approach.

A series of novel alkyl derivatives () and 1-1,2,3-triazole analogues () of Meldrum's acid were synthesized in a highly effective way by using chemistry and screened for in vitro -glucosidase inhibitory activity to examine their antidiabetic potential. H NMR, C-NMR, and high-resolution electrospray ionization mass spectra (HR-ESI-MS) were used to analyze each of the newly synthesized compounds. Interestingly, these compounds demonstrated high to moderate α-glucosidase inhibitory potency having an IC range of 4.

Discovery of New Boswellic Acid Hybrid 1-1,2,3-Triazoles for Diabetic Management: In Vitro and In Silico Studies.

A series of 24 new 1-1,2,3-triazole hybrids of 3--acetyl-11-keto-β-boswellic acid (β-AKBA ()) and 11-keto-β-boswellic acid (β-KBA ()) was designed and synthesized by employing "click" chemistry in a highly efficient manner. The 1,3-dipolar cycloaddition reaction between β-AKBA-propargyl ester intermediate or β-KBA-propargyl ester intermediate with substituted aromatic azides in the presence of copper iodide (CuI) and Hünig's base furnished the desired products-1-1,2,3-triazole hybrids of β-AKBA () and β-KBA ()-in high yields. All new synthesized compounds were characterized by H-, C-NMR spectroscopy, and HR-ESI-MS spectrometry.

Bio-oriented synthesis of ibuprofen derivatives for enhancement efficacy in post-operative and chronic inflammatory pain models.

The discovery of post-operative, chronic inflammatory pain and any gastroulcerogenic potential using well-established animal models with new structures, high efficiency, broad-spectrum, and low toxicity has been the focus of medicinal chemists. In the present article, we are reporting the design and synthesis of various derivatives of ibuprofen by modifying the carboxyl group of ibuprofen using three steps reactions; esterification under microwave-irradiation in 10 minutes, hydrazide formation, and finally schiff's base reaction. Microwave-assisted esterification reaction can be employed to quickly explore and increase molecular diversity in synthetic chemistry.

Nanotechnology in combating biofilm: A smart and promising therapeutic strategy.

Since the birth of civilization, people have recognized that infectious microbes cause serious and often fatal diseases in humans. One of the most dangerous characteristics of microorganisms is their propensity to form biofilms. It is linked to the development of long-lasting infections and more severe illness.

Biochemical and inhibition of bovine and human carbonic anhydrase-II by 1H-1,2,3-triazole analogs.

A series of 1H-1,2,3-triazole analogs (7a-7d and 9a-9s) were synthesized via "click" chemistry and evaluated for carbonic anhydrase-II (bovine and human) inhibitory activity. The synthesis of intermediates, 7a and 7c, was achieved by using (S)-(-)ethyl lactate as a starting material. These compounds (7a and 7c) underwent Suzuki-Miyaura cross-coupling reaction with different arylboronic acids in 1,4-dioxane, reflux at 90-120°C for 8 h using Pd(PPh) as a catalyst (5 mol%), and KCO (3.

Synthesis and antidepressant-like effects of new 5-epi-incensole and 5-epi- incensole acetate in chronic unpredictable mild stress model of depression; behavioural and biochemical correlates.

In the current investigation, 5-epi-incensole (3) and 5-epi-incensole acetate (5) were synthesized from the most potent anti-depressant constituents incensole (1) and incensole acetate (2) of Boswellia papyrifera Hochst. The resulting compounds were evaluated for their ability to ameliorate depressive symptoms in forced swim test (FST) and tail suspension test (TST) in chronic unpredictable mild stress (CUMS) induced depression paradigm. The results demonstrated that compounds 3 and 5 at the doses of 1 and 3 mg/kg administered for 28 days, significantly reduced the immobility time in FST and TST and were devoid of any effect on locomotor activity in the open field test (OFT).

Virtual 2D map of cyanobacterial proteomes.

Cyanobacteria are prokaryotic Gram-negative organisms prevalent in nearly all habitats. A detailed proteomics study of Cyanobacteria has not been conducted despite extensive study of their genome sequences. Therefore, we conducted a proteome-wide analysis of the Cyanobacteria proteome and found Calothrix desertica as the largest (680331.

Exploring Dose-Dependent Cytotoxicity Profile of Mediated Green Synthesized Silver Nanoparticles against MDA-MB-231 Breast Carcinoma.

Green-based synthesis of metal nanoparticles using marine seaweeds is a rapidly growing technology that is finding a variety of new applications. In the present study, the aqueous extract of a marine seaweed, , was employed for the synthesis of metallic nanoparticles without using any reducing and stabilizing chemical agents. The visual color change and validation through UV-Vis spectroscopy provided an initial confirmation regarding the -mediated green synthesized silver nanoparticles.

Edible Mushrooms as Novel Myco-Therapeutics: Effects on Lipid Level, Obesity and BMI.

Obesity, usually indicated by a body mass index of more than 30 kg/m, is a worsening global health issue. It leads to chronic diseases, including type II diabetes, hypertension, and cardiovascular diseases. Conventional treatments for obesity include physical activity and maintaining a negative energy balance.

Exploring the Bioactive Potentials of C-AgNPs Nano-Composites against Malignancies and Microbial Infections.

At present, the potential role of the AgNPs/endo-fullerene molecule metal nano-composite has been evaluated over the biosystems in-vitro. The intra-atomic configuration of the fullerene molecule (C) has been studied in-vitro for the anti-proliferative activity of human breast adenocarcinoma (MDA-MB-231) cell lines and antimicrobial activity against a few human pathogens that have been augmented with the pristine surface plasmonic electrons and antibiotic activity of AgNPs. Furthermore, FTIR revealed the basic vibrational signatures at ~3300 cm, 1023 cm, 1400 cm for O-H, C-O, and C-H groups, respectively, for the carbon and oxygen atoms of the C molecule.

Naturally Occurring O-Heterocycles as Anticancer Agents.

Cancer is a leading cause of death worldwide. Proper efficient drugs are required to treat this deadly disease. Natural products have long been a vital source of anticancer agents and they have generated various "lead compounds" suitable for drug developments.

Synthesis and antimicrobial activity of 1-1,2,3-triazole and carboxylate analogues of metronidazole.

Herein, a series of novel 1-1,2,3-triazole and carboxylate derivatives of metronidazole ( and ) were synthesized and evaluated for their antimicrobial activity in vitro. All the newly synthesized compounds were characterized by H NMR, C NMR, HRMS, and F NMR (, and ) spectroscopy wherever applicable. The structures of compounds , and were unambiguously confirmed by single crystal X-ray analysis diffraction method.

Cembranoids from Boswellia species.

Frankincense of Boswellia species has long been used in traditional medicines, mainly for its interesting anti-inflammatory and anti-depressant properties of its di- and triterpenes. Boswellic acids (triterpenes) and cembranoids (diterpenes) are the major constituents of frankincense from all reported species which are responsible for the overall biological activity of frankincense. Boswellic acids have been thoroughly investigated for decades but cembranoids have attracted considerable attention only recently, and a good number of publications have highlighted the important role of these 14-membered rings in contributing to the superior anti-inflammatory activity of the sacred resin.

Synthesis of New 1-1,2,3-Triazole Analogs in Aqueous Medium "" Chemistry: A Novel Class of Potential Carbonic Anhydrase-II Inhibitors.

A series of novel 1-1,2,3-triazole analogs () were synthesized chemistry and Suzuki-Miyaura cross-coupling reaction in aqueous medium. The compounds were evaluated for their carbonic anhydrase-II enzyme inhibitory activity . The synthesis of triazole was accomplished using ()-(-) ethyl lactate as a starting material.

Heterogeneous Pd/C-catalyzed, ligand free Suzuki-Miyaura coupling reaction furnishes new -terphenyl derivatives.

A series of new -terphenyls derivatives have been efficiently synthesized by a ligand-free heterogeneous Pd/C-catalyzed two-fold Suzuki-Miyaura coupling reaction. Methyl 5-bromo-2-iodobenzoate was selected to react with a variety of different aryl boronic acids (). Nine new -terphenyl derivatives (-) were prepared and the structures were confirmed by several analytical techniques including infrared, spectroscopy, H and C NMR spectroscopy, mass spectrometry, and in the case of compound by X-ray diffraction method.

Recent Advances in the Stereoselective Total Synthesis of Natural Pyranones Having Long Side Chains.

Pyranone natural products have attracted great attention in recent years from chemists and biologists due to their fascinating stereoisomeric structural features and impressive bioactivities. A large number of stereoselective total syntheses of these compounds have been described in the literature. The natural pyranones with long side chains have recently received significant importance in the synthetic field.

Synthesis of novel (R)-4-fluorophenyl-1H-1,2,3-triazoles: A new class of α-glucosidase inhibitors.

Diabetes is a non-communicable disease, which occurs either due to the lack of insulin or the inability of the human body to recognize it. The recent data indicates an increase in the trend of people diagnosed with Type 2 diabetes mellitus (T2DM). α-Glucosidase inhibitors are known to reduce the impact of carbohydrates on blood glucose level and prevent the digestion of carbohydrates.

Synthesis of 1H-1,2,3-triazole derivatives as new α-glucosidase inhibitors and their molecular docking studies.

Inhibition of α-glucosidase is an effective strategy for controlling the post-prandial hyperglycemia in diabetic patients. For the identification of new inhibitors of this enzyme, a series of new (R)-1-(2-(4-bromo-2-methoxyphenoxy) propyl)-4-(4-(trifluoromethyl) phenyl)-1H-1,2,3-triazole derivatives were synthesized (8a-d and 10a-e). The structures were confirmed by NMR, mass spectrometry and, in case of compound 8a, by single crystal X-ray crystallography.