Category: CBL Articles

We report the synthesis and characterization of a series of metal complexes of bivalent Cobalt, Nickel, Copper, Zinc and Palladium with novel Schiff base ligand 4-((4-isopropoxybenzylidene)amino)-5-propyl-4H-3-thiol-1,2,4-triazole (IBPT). The ligand (IBPT) was derived by the condensation reaction of 4-isopropoxybenzaldehyde and 4-amino-5-propyl-3-thiol-1,2,4-triazole and characterised by IR and proton(¹H) NMR spectroscopic techniques. The complexes have been investigated using characterised Fourier transform infrared (FT-IR), nuclear magnetic resonance (NMR), electron spin resonance (ESR), UV−visible and fluorescence spectroscopies. Based on the comparative analysis of IR and NMR data of ligand and metal complexes, it has been suggested that the ligand chelates with metal ions in a bidentate fashion via N (azomethine) and S (thiol) atoms. Elemental analysis, molar conductance, magnetic moments and redox behaviour of complexes have also been studied. In addition, Tauc’s formula has been employed to determine the optical bandgap of complexes using the electronic spectral data. Thermogravimetric analysis revealed the number of coordinated water molecules and thermal stability of metal complexes. Various thermodynamic and kinetic parameters have been evaluated with the help of thermal data using Coats- Redfern method. The octahedral environment of divalent Cobalt, Nickel and Zinc complexes while square planner structure of Copper and Palladium complexes was elucidated with the help of spectroscopic data. Moreover, in-vitro antimicrobial activities of Schiff base ligand and its complexes were estimated against four pathogenic bacterial (two Gram Positive, two Gram negative) and three fungal strains (C. Albicans, A. Niger and A. Clavatus). The biological outcomes ensure the convenient utility of these novel complex as antimicrobial agents.

URN:NBN:sciencein.cbl.2022.v9.407

Intracerebral haemorrhage is the condition of bleeding inside the brain, either spontaneous or traumatic. Though this form of stroke accounts to only about 15% of the cases, the mortality rate is the highest. People with stroke associated with ICH very rarely regain functional independence. The post-stroke complications are due to the extending loss of vascular integrity leading to prolonged secondary inflammation. Early detection of biomarkers associated with the condition and the efficacy of these biomarkers to depict the prognostic rate become essential tools for the clinicians to handle patients with ICH. Development of in vivo models that can simulate the intricate pathophysiology of the condition can add up new biomarkers that serve diagnostic and prognostic purposes.

URN:NBN:sciencein.cbl.2022.v9.408

The synthesis of novel 1,2,3-triazoles of Nilutamide (4a–4n) via Cu(I)-promoted 1,3-dipolar cycloaddition reaction between several terminal alkynes and 1-(3-azidopropyl)-5,5-dimethyl-3-(4-nitro-3-(trifluoromethyl)phenyl)imidazolidine-2,4-dione have been reported herein. In vitro anticancer activity studies of these synthesized compounds over two human prostate cell lines PC3 and DU-145 revealed that the compounds 4c, 4f and 4n exhibit slightly greater activity against two cell lines than the standard etoposide. Predominantly, the compound 4f displayed excellent activity over PC3 and DU-145 having IC₅₀ values of 1.84and 1.34 μM respectively. The three most potent compounds 4c, 4f and 4n were also investigated for their inhibitory potential against tyrosine kinase EGFR and found that compound 4f showed superior activity than the standard erlotinib, while remaining two compounds 4c and 4n showed comparable activity with the standard.

URN:NBN:sciencein.cbl.2022.v9.405

We report the synthesis and characterization of a series of metal complexes of bivalent Cobalt, Nickel, Copper, Zinc and Palladium with novel Schiff base ligand 4-((4-isopropoxybenzylidene)amino)-5-propyl-4H-3-thiol-1,2,4-triazole (IBPT). The ligand (IBPT) was derived by the condensation reaction of 4-isopropoxybenzaldehyde and 4-amino-5-propyl-3-thiol-1,2,4-triazole and characterised by IR and proton(¹H) NMR spectroscopic techniques. The complexes have been investigated using characterised Fourier transform infrared (FT-IR), nuclear magnetic resonance (NMR), electron spin resonance (ESR), UV−visible and fluorescence spectroscopies. Based on the comparative analysis of IR and NMR data of ligand and metal complexes, it has been suggested that the ligand chelates with metal ions in a bidentate fashion via N (azomethine) and S (thiol) atoms. Elemental analysis, molar conductance, magnetic moments and redox behaviour of complexes have also been studied. In addition, Tauc’s formula has been employed to determine the optical bandgap of complexes using the electronic spectral data. Thermogravimetric analysis revealed the number of coordinated water molecules and thermal stability of metal complexes. Various thermodynamic and kinetic parameters have been evaluated with the help of thermal data using Coats- Redfern method. The octahedral environment of divalent Cobalt, Nickel and Zinc complexes while square planner structure of Copper and Palladium complexes was elucidated with the help of spectroscopic data. Moreover, in-vitro antimicrobial activities of Schiff base ligand and its complexes were estimated against four pathogenic bacterial (two Gram Positive, two Gram negative) and three fungal strains (C. Albicans, A. Niger and A. Clavatus). The biological outcomes ensure the convenient utility of these novel complex as antimicrobial agents.

URN:NBN:sciencein.cbl.2022.v9.407

Cancer is one of the most fatal diseases of recent times that causes several deaths every year. The disease variations in different parts of the world, the impact of available medical facilities, and other socio-economic factors have impacted the proper management of this disease. The comparative statistical data of cancer types like breast, prostate, colon, lung, lymph, blood, brain, and kidney cancers can be used to design treatment strategies and therapeutics development. With the advancement of science, several drugs besides diagnostic methods have emerged to control respective cancer and have assisted in curing this disease to some extent. The comparative statistics analysis for cancer about current prevalence is included here to bring a clear framework for the efforts towards future drug development to manage this disease. The availability of new diagnostics and therapeutics and advanced medical facilities in clinics impact cancer statistics. An evaluation of current trends and statistics of cancer pathology vis-à-vis theranostics (diagnostics as well as therapeutics) progress with possible application in clinical settings constitutes the core part of the discussion in this review.

URN:NBN:sciencein.cbl.2023.v10.451

Intracerebral haemorrhage is the condition of bleeding inside the brain, either spontaneous or traumatic. Though this form of stroke accounts to only about 15% of the cases, the mortality rate is the highest. People with stroke associated with ICH very rarely regain functional independence. The post-stroke complications are due to the extending loss of vascular integrity leading to prolonged secondary inflammation. Early detection of biomarkers associated with the condition and the efficacy of these biomarkers to depict the prognostic rate become essential tools for the clinicians to handle patients with ICH. Development of in vivo models that can simulate the intricate pathophysiology of the condition can add up new biomarkers that serve diagnostic and prognostic purposes.

URN:NBN:sciencein.cbl.2022.v9.408

The synthesis of novel 1,2,3-triazoles of Nilutamide (4a–4n) via Cu(I)-promoted 1,3-dipolar cycloaddition reaction between several terminal alkynes and 1-(3-azidopropyl)-5,5-dimethyl-3-(4-nitro-3-(trifluoromethyl)phenyl)imidazolidine-2,4-dione have been reported herein. In vitro anticancer activity studies of these synthesized compounds over two human prostate cell lines PC3 and DU-145 revealed that the compounds 4c, 4f and 4n exhibit slightly greater activity against two cell lines than the standard etoposide. Predominantly, the compound 4f displayed excellent activity over PC3 and DU-145 having IC₅₀ values of 1.84and 1.34 μM respectively. The three most potent compounds 4c, 4f and 4n were also investigated for their inhibitory potential against tyrosine kinase EGFR and found that compound 4f showed superior activity than the standard erlotinib, while remaining two compounds 4c and 4n showed comparable activity with the standard.

URN:NBN:sciencein.cbl.2022.v9.405

A new series of quinoxaline linked 1,2,4-triazole sulfonamide  derivatives were designed and efficiently synthesized. All compounds were characterized by their IR, ¹HNMR, ¹³CNMR, and Mass spectral data, and elemental analysis. The final compounds (5a-m) were screened for in vitro anti-proliferative activity against cancer cell lines HeLa (lung), A549 (carcinoma), MCF-7 (breast) and HCT116 (colon).The  results revealed that the compounds 5k, 5l and 5d have shown promising activity as compared to etoposide. Predominantly, the compound 5k displayed greater activity on HeLa, A549, MCF-7and HCT116 with IC₅₀ values of 1.97±0.09, 1.84±0.07, 3.10±0.04and 4.10±0.07 than the standard drug etoposide. Moreover, molecular docking studies of 5k, 5l and 5d on EGFR receptor suggested that the most potent compound 5k strongly binds to protein EGFR (pdbid: 4HJO). Furthermore, the compounds 5k and 5l displayed promising inhibitory activity over tyrosine kinase EGFR when compared with the standard erlotinib.

Dibenzofuran is an important heterocyclic compound and is an important part of various natural compounds. There are various medicinal compounds containing dibenzofurans, sold in the market to combat different human diseases and plant infections. Research on dibenzofuran is an advancing field in the medicinal science. Several compounds are under the clinical trials and are expected to be utilized in various treatments. This review article encompasses various advancements in the study of these dibenzo derivatives. The biological activity of these scaffolds hovering around cytotoxicity of the cells, bacterial infections, fungal infections, type-2 diabetes, platelet coagulation and in the effective skin treatment, has been discussed in the following article.  The toxicology of the compound is also argued and selected biological applications are hereby discussed to make easier for the researchers to have a consolidated sight over the topic.

The growth of amyloid β peptides arises from inappropriate cleavage of amyloid precursor protein that induces the formation of amyloid plaques in the brain. An excessive accumulation of amyloid β plaques promotes the development of dementia, specifically Alzheimer’s disease (AD). Histopathological evidence suggested that insulin resistance and type 2 diabetes condition have a stronger correlation with Alzheimer’s disease development. An increasing concentration of amyloid β leads to impaired binding of insulin to its receptor. Previous studies suggested that the monomeric form of amyloid β was the potential molecule, which can compete with insulin for receptor binding. The objective of this work was to study the molecular interactions of insulin and amyloid β to insulin receptors using protein-protein docking and molecular dynamics Simulations. Analysis of docked complexes suggested that there are common insulin receptor residues for insulin and amyloid β binding. Further molecular dynamics Simulations study reveals that the monomeric form of amyloid β interacts with a similar set of receptor residues as observed in the insulin-insulin receptor complex.