Polymers and their composites have recently attracted attention in both pharmaceutical and biomedical applications. Polyethylene glycol (PEG) is a versatile polymer extensively used in medicine. Herein, three novel PEG-based polymers that are pseudopolyrotaxane (PEG/α-CD) (1), titania–nanocomposite (PEG/TiO2NPs) (2), and pseudopolyrotaxane–titania–nanocomposite (PEG/α-CD/TiO2NPs) (3), were synthesized and characterized. The chemical structure, surface morphology, and optical properties of the newly materials were examined by FT-IR, 1H-NMR, SEM, and UV–Vis., respectively. The prepared polymers were used as drug carriers of sulfaguanidine as PEG/α-CD/Drug (4), PEG/TiO2NPs/Drug (5), and PEG/α-CD/TiO2NPs/Drug (6). The influence of these drug-carrying formulations on the physical and chemical characteristics of sulfaguanidine including pharmacokinetic response, solubility, and tissue penetration was explored. Evaluation of the antibacterial and antibiofilm effect of sulfaguanidine was tested before and after loading onto the prepared polymers against some Gram-negative and positive bacteria (E. coli, Pseudomonas aeruginosa, and Staphylococcus aureus (MRSA)), as well. The results of this work turned out to be very promising as they confirmed that loading sulfaguanidine to the newly designed polymers not only showed superior antibacterial and antibiofilm efficacy compared to the pure drug, but also modified the properties of the sulfaguanidine drug itself.
Interlocked molecules such as rotaxanes and catenanes have a lot of studies in last twenty years. Due to their unique structures and properties. In this work [2] rotaxanes (A), (B), and (C) containing of α, β and/or γ cyclodextrins have been prepared respectively. Construction of these compounds depend on forming stable inclusion complexes between cyclodextrin and hexamethylenediamine which ended with a bulky group 9,10-dihydro-9,10-ethanoanthracene-11,12-dicarboxylic anhydride. The chemical structure of synthesized inclusion complexes can be confirmed by spectral analysis and physical properties.
Reaction of isonicotinaldehyde with 2-cyanoacetohydrazide afforded (E)-2-cyano-N'-(pyridin-4-ylmethylene)acetohydrazide (1). Compound 1 was used as the precursor for the synthesis of novel pyridine derivatives by reaction with different arylidene malononitriles, malononitrile and acetylacetone to give pyridine derivatives 5a-e, 6 and 7, respectively. 4,4'-Bipyridine derivatives 9a-d were synthesized by a three-component reaction of isonicotinaldehyde, 2-cyanoacetohydrazide and activated nitriles 8a-d. Treatment of compound 9a with different aromatic aldehydes gave [1,2,4] triazolo[1,5-a]pyridine derivatives 11a-c. All reaction products were characterized by analytical and spectral data. For the novel compounds their bioactivity as antitumor agents was examined for in vitro cytotoxicity against HepG-2 and MCF-7. It was found that compounds 9a and 9b have high cytotoxic activity against both HepG-2 and MCF-7.
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