Experimental and computational modeling of the biological activity of benzaldehyde sulphur trioxide as a potential drug for the treatment of Alzheimer disease

Synthesis, spectral characterization, lethal dose (LD50) and acute toxicity studies of 1,4-Bis(imidazolylazo)benzene (BIAB).

Azo molecules, characterized by the presence of a -N=N- double bond, are widely used in various fields due to their sensitivity to external stimuli, ch as light. The emergence of bacterial resistance has pushed research towards designing new antimicrobial molecules that are more efficient than those currently in use. Many authors have attempted to exploit the antimicrobial activity of azobenzene and to utilize their photoisomerization for selective control of the bioactivities of antimicrobial molecules, which is necessary for antibacterial therapy. This review will provide a systematic and consequential approach to coupling azobenzene moiety with active antimicrobial molecules and drugs, including small and large organic molecules, such as peptides. A selection of significant cutting-edge articles collected in recent years has been discussed, based on the structural pattern and antimicrobial performance, focusing especially on the photoactivity of azobenzene and the design of smart materials as the most targeted and desirable application.

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Azobenzene as Antimicrobial Molecules

In the present study, a series of azo derivatives (TR-1 to TR-9) have been synthesised via the diazo-coupling approach between substituted aromatic amines with phenol or naphthol derivatives. The compounds were evaluated for their therapeutic applications against alpha-glucosidase (anti-diabetic) and pathogenic bacterial strains E. coli (gram-negative), S. aureus (gram-positive), S. aureus (gram-positive) drug-resistant strain, P. aeruginosa (gram-negative), P. aeruginosa (gram-negative) drug-resistant strain and P. vulgaris (gram-negative). The IC50 (µg/mL) of TR-1 was found to be most effective (15.70 ± 1.3 µg/mL) compared to the reference drug acarbose (21.59 ± 1.5 µg/mL), hence, it was further selected for the kinetic studies in order to illustrate the mechanism of inhibition. The enzyme inhibitory kinetics and mode of binding for the most active inhibitor (TR-1) was performed which showed that the compound is a non-competitive inhibitor and effectively inhibits the target enzyme by binding to its binuclear active site reversibly.

Diaryl azo derivatives as anti-diabetic and antimicrobial agents: synthesis, in vitro , kinetic and docking studies.

Conventional antimicrobial agents are losing the war against drug resistance day-by-day. Chitosan biopolymer is one of the alternative materials that lends itself well to this application by fine-tuning its bioactivity using different pendant groups. Herein, we report the synthesis of novel chitosan with pendant (E)-5-((4-acetylphenyl)diazenyl)-6-aminouracil (APAU) groups by forming Schiff base linkages between chitosan and the pendant groups. These chitosan biopolymers with pendant APAU groups form films superior in thermal stability compared to the neat chitosan. Interestingly, APAU alone was inactive against K. pneumoniae, E. coli, S. aureus, T. rubrum and C. albicans. However, novel chitosan samples were active against S. aureus with an MIC of 390 μg mL-1, half that of plain chitosan at 780 μg mL-1. APAU modified chitosan samples, CA80 and CA100 showed an MIC (against K. pneumoniae and E. coli) of 23.4 μg mL-1, superior to plain chitosan's MIC of 187.5 μg mL-1 and is close to commercial Fluconazole's MIC of 11.7 μg mL-1. The activity of chitosan changes with APAU content and at higher concentrations shows a strong synergetic antimicrobial effect.

Hadjira Berredjem

Papers

Synthesis, characterization and antimicrobial activity of some new azo dyes derived from 4-hydroxy-6-methyl-2H-pyran-2-one and its dihydro derivative