Synthesis of Chloro-Substituted 6&lt;i&gt;H&lt;/i&gt;-Dibenzo[&lt;i&gt;b&lt;/i&gt;,&lt;i&gt;d&lt;/i&gt;]pyran-6-one Natural Products, Graphislactone G, and Palmariols A and B

The interaction of drugs with proteins plays a very important role in the distribution of the drug. Human serum albumin (HSA) is the most abundant protein in the human body and showing great binding characteristics has gained a lot of importance pharmaceutically. It plays an essential role in the pharmacokinetics of a number of drugs and hence several reports are available on the interaction of drugs with HSA. It can bind to cancer drugs and thus it is crucial to look at the binding characteristics of these drugs with HSA. Herein we summarize the binding properties of some anti-cancer drugs by specifically looking into the binding site with HSA. The number of drugs binding at Sudlow's site I situated in subdomain II A is more than the drugs binding at Sudlow's site II.

show abstract

Design, synthesis, and unraveling the antibacterial and antibiofilm potential of 2-azidobenzothiazoles: insights from a comprehensive in vitro study

Qadir,

Kanth,

Aasif

et al. 2023

Front. Chem.

View full text Add to dashboard Cite

The present study reports the synthesis of 2-azidobenzothiazoles from substituted 2-aminobenzothiazoles using sodium nitrite and sodium azide under mild conditions. All the synthesized compounds were examined for their antibacterial activity against Gram (+) bacteria, Staphylococcus aureus (ATCC 25923), Enterococcus faecalis (ATCC 51299), Bacillus cereus (ATCC 10876) and Gram (−) bacteria, Escherichia coli (ATCC 10536), Pseudomonas aeruginosa (ATCC 10145), Klebsiella pneumonia (ATCC BAA-2146)and clinical isolates of Gram (+) Methicillin Resistant S. aureus (MRSA) and Multi Drug Resistant E. coli. The Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC) values by broth dilution method revealed that compound 2d exhibited significant antibacterial potential against E. faecalis and S. aureus with MIC of 8 μg/mL, while other synthesized compounds had only moderate effects against all the tested species. The compound significantly inhibited the biofilm formation of the bacterial strains below its MIC. The selective cytotoxicity of Compound 2d towards bacterial cells was evidenced on extended exposure of Human Embryonic Kidney-293 cell line to higher concentrations of the compound. Hence, the present study confirmed that compound 2d can be a potential drug candidate for future development as an antibacterial drug.

show abstract

Synthesis of Chloro-Substituted 6<i>H</i>-Dibenzo[<i>b</i>,<i>d</i>]pyran-6-one Natural Products, Graphislactone G, and Palmariols A and B

Cited by 3 publications

References 57 publications

Six-membered ring systems: with O and/or S atoms

Six-membered ring systems: with O and/or S atoms

Site-Specific Binding of Anti-Cancer Drugs to Human Serum Albumin

Design, synthesis, and unraveling the antibacterial and antibiofilm potential of 2-azidobenzothiazoles: insights from a comprehensive in vitro study

Contact Info

Product

Resources

About