In vivo imaging of pyrrole-imidazole polyamides with positron emission tomography

The biodistribution profiles in mice of two pyrrole-imidazole polyamides were determined by PET. Pyrrole-imidazole polyamides are a class of small molecules that can be programmed to bind a broad repertoire of DNA sequences, disrupt transcription factor-DNA interfaces, and modulate gene expression pathways in cell culture experiments. The 18F-radiolabeled polyamides were prepared by oxime ligation between 4-[18F]-fluorobenzaldehyde and a hydroxylamine moiety at the polyamide C terminus. Small animal PET imaging of radiolabeled polyamides administered to mice revealed distinct differences in the biodistribution of a 5-ring β-linked polyamide versus an 8-ring hairpin, which exhibited better overall bioavailability. In vivo imaging of pyrrole-imidazole polyamides by PET is a minimum first step toward the translation of polyamide-based gene regulation from cell culture to small animal studies

Silicon containing electroconductive polymers and structures made therefrom

An electropolymerized film comprised of polymers and copolymers of a monomer is formed on the surface of an anode. The finished structures have superior electrical and mechanical properties for use in applications such as electrostatic dissipation and for the reduction of the radar cross section of advanced aircraft

Soluble poly-3-alkylpyrrole polymers on films and fabrics

Conductive textiles with specific properties can be produced by the chemical polymerisation of a range of 3-alkylpyrroles in the presence of textiles. The morphologies of these coatings are altered from the traditional conductive coatings. Comparison using a SEM reveals substantial differences.<br /

Flexible synthesis of polyfunctionalised 3-fluoropyrroles

An efficient and selective approach for the synthesis of polyfunctionalised 3-fluoropyrroles has been developed starting from commercial aldehydes. The methodology is concise, efficient and allows for the modular and systematic assembly of polysubstituted 3-fluoropyrroles. This synthesis provides an alternative and highly convergent strategy for the generation of these chemically and biologically important units

Green synthesis of highly functionalized octahydropyrrolo[3,4-c]pyrrole derivatives using subcritical water, and their anti(myco)bacterial and antifungal activity

A series of novel 2-(thiazol-2-yl)-octahydropyrrolo[3,4-c]pyrroles was synthesized by reaction of octahydropyrrolo[3,4-c]pyrrole N-benzoylthiourea derivatives and α-haloketones in subcritical water at 130 °C in 75-91% yield. Both the thiourea intermediates and the end productswere synthesized in subcritical water, which proved a suitable green alternative to acetone by delivering the desired compounds in much shorter reaction times and practically the same yields. The antimicrobial activity of the compounds was determined against five bacterial strains and three fungal strains, and MIC values of 15.62-250 µg/mL were observed. Moreover, the compounds exhibited antimycobacterial activity against M. tuberculosis H37Rv with MIC values of 7.81-62.5 μg/mL

Labeless and reversible immunosensor assay based upon an electrochemical current-transient protocol

A novel labeless and reversible immunoassay based upon an electrochemical current-transient protocol is reported which offers many advantages in comparison to classical immuno-biochemical analyses in terms of simplicity, speed of response, reusability and possibility of multiple determinations. Conducting polypyrrole films containing antibodies against 1) Bovine Serum Albumin (BSA) and 2) Digoxin were deposited on the surface of platinum electrodes to produce conductive affinity matrices having clearly defined binding characteristics. The deposition process has been investigated using 125I labelled anti-digoxin to determine optimal fabrication protocols. Antibody integrity and activity, together with non-specific binding of antigen on the conducting matrix have also been investigated using tritiated digoxin to probe polypyrrole/anti-digoxin films. Amperometric responses to digoxin were recorded in flow conditions using these films, but the technique was limited in use mainly due to baseline instability. Anti-BSA - polypyrrole matrices were investigated in more detail in both flow and quiescent conditions. No observable response was found in flow conditions, however under quiescent conditions (in non-stirred batch cell), anti-BSA – polypyrrole films have been demonstrated to function as novel quantitative chronoamperometric immuno-biosensors when interrogated using a pulsed potential waveform. The behaviour of the electrodes showed that the antibody/antigen binding and/or interaction process underlying the response observed was reversible in nature, indicating that the electrodes could be used for multiple sensing protocols. Calibration profiles for BSA demonstrated linearity for a concentration range of 0-50 ppm but tended towards a plateau at higher concentrations. Factors relating to replicate sensor production, sample measurement and reproducibility are discuss