The antibacterial activity of the S-unsubstituted- and S-benzyl-substituted-2-mercapto-benzothiazoles 1-4 has been evaluated after complexation with Methyl-β-Cyclodextrin (Me-β-CD) or incorporation in solid dispersions based on Pluronic® F-127 and compared with that of the pure compounds. This with the aim to gain further insights on the possible mechanism(s) involved in the CD-mediated enhancement of antimicrobial eﬀectiveness, a promising methodology to overcome the microbial resistance issue. Together with Diﬀerential Scanning Calorimetry, FT-IR spectroscopy and X-ray Powder Diﬀraction investigations, a molecular modeling study focused on compounds 2 and 4 showed that the S-unsubstituted compound 2/Me-β-CD complex should be more stable than S-benzyl-substituted 4/Me-β-CD. Only for 1/Me-β-CD or, particularly, 2/Me-β-CD complexes, the antibacterial eﬀectiveness was enhanced in the presence of selected bacterial strains. The results herein presented support the mechanisms focusing on the interactions of the bacterial membrane with CD complexes more than those focusing on the improvement of dissolution properties consequent to CD complexation.
|Titolo:||Effect of Methyl -β- Cyclodextrin on the antimicrobial activity of a new series of poorly water-soluble benzothiazoles|
CORBO, Filomena Faustina Rina (Corresponding)
|Data di pubblicazione:||2019|
|Appare nelle tipologie:||1.1 Articolo in rivista|