Background
The o-phenylenediamine is a versatile starting material for several compounds. Synthesized o-phenylenediamine and amino acids (glycine, alanine, aspartic acid, and l-proline) undergo condensation via Phillips reaction. The synthesized compound showed the promising antibacterial activity of Bacillus subtilis and Pseudomonas aeruginosa at the concentration of 100, 50, 25, 12.5, 6.25, 3.12, 1.6, 0.8, 0.4, and 0.2 μg/ml. Ciprofloxacin was used as standard drug. Synthesis of benzimidazole derivatives was carried out and purified by recrystallization process using ethanol. Substituted derivatives were characterized by melting point, TLC and spectroscopic methods include FT-IR and 1H-NMR.
Results
In silico studies were adopted for synthetic derivatives by Molinspiration, ChemDraw, and online software tool. Minimum inhibitory concentration (MIC) values of B. subtilis and P. aeruginosa were reported, and benzimidazole ligands and Molinspiration scores were generated and listed.
Conclusion
The more negative values indicate a higher binding affinity. The generated ligand observations can be visualized. Physical constants of synthesized derivates such as solubility and melting point were determined. Bioactivity scores were noted for different derivatives and predicted percentage absorption in the gut. The antibacterial activity was performed using the MIC method (aerobic).
A novel scaffolds of stilbene were identified as inhibitors of Mycobacterium tuberculosis by targeting the nucleoid-associated protein, HU, using molecular docking. Based on the proposed combinatorial library I to VI,...
Introduction
Tuberculosis (TB) patients on the National Tuberculosis Elimination Program (NTEP) treatment protocol receive daily doses without health professional‐supervised drug intake as during the previous directly observed treatment short‐course (DOTS) regimen. We aimed to measure the level of adherence to anti‐tubercular treatment (ATT) and the reasons for non‐adherence among drug‐sensitive TB patients on a daily‐dose regimen in South India.
Methods
A cross‐sectional study was conducted among TB patients who received ATT as part of the standard treatment protocol in NTEP. Patients were interviewed to capture their understanding of TB, adherence, and the reason for non‐adherence to ATT using validated instruments. Urine drug metabolite testing was performed using the high‐performance liquid chromatography (HPLC) technique to confirm adherence.
Results
A total of 488 patients were recruited for the study. 64.8% of patients had ‘good knowledge’ about TB and ATT. According to the subjective report, 63.7% of patients were adherent, but urine drug metabolite testing revealed 53.4% adherence. A statistically significant difference (p < 0.05) exists between subjective and objective adherence measures. Patient‐reported reasons for non‐adherence were side effects of ATT (18.6%), loss of daily wages (15.0%), and forgetfulness (10.0%), among others.
Conclusions
Nearly half of the patients were non‐adherent to the daily dosing regimen. Adherence as reported by the patients is unreliable, and urine testing could be used in routine care to assess adherence.
Clinical Trial Registration and Number
CTRI/2020/04/024941.
Various biologically important Stilbene analogues were competently synthesized using inexpensive, non-toxic, and readily available amino acids and Stilbene; the systematic study was carried out to characterize parameters such as TLC, melting point, IR, 1H NMR and mass spectral studies. The synthesized compounds were screened for anticancer activities. The molecular docking studies have been performed by using software Autodock 4.2, Autodock vina. The targeted proteins are P450a2 & Estrogen.
The reaction of phenylacetic acid substituted Benzaldehyde, and triethylamine in acetic anhydride was irradiated in a microwave oven for 3 minutes at 700W afforded (2E)-3-(substituted phenyl)-2-phenylacrylic acid. The above compound, after irradiating with hydrazine provided (2E)-3-(substituted phenyl)-2-phenyl acrylic acid hydrazide. Anti-Cancer activity for synthesized compounds was evaluated using the MTT assay technique against colon cancer. The results were obtained as a percentage in cell lysis data. The IC50 value of the compounds was between 0.037-0.0257 µM/lt. Among all the compounds, tyrosine derivatives exhibited the more potent activity. Insilico studies PCB-arg having more binding affinity with the receptor Cytochrome P450 A2 and PCB-try having more binding affinity with the receptor estrogen beta when compared to other derivatives.
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