The phosphorylated and thiophosphorylated benzothiazole derivatives have been synthesized by the reaction of phosphorus oxychloride/phosphorus thiochloride with 2-(2 -aminophenyl)benzothiazole in 1:1, 2:1, 3:1, and 1:2 molar ratios in presence of triethylamine. Plausible structures have been proposed on the basis of elemental analysis IR, 1 H NMR, 31 P NMR, and mass spectral studies. The fungicidal activity of these derivatives have been evaluated against pathogenic fungi Aspergillus niger and Fusarium oxysporium. The fungicidal data reveals that these compounds are more fungitoxic than the parent 2-(2 -aminophenyl)benzothiazole compound.
Aggregates of therapeutic proteins have been associated with increased immunogenicity in pre-clinical models as well as in human patients. Recent studies to understand aggregates and their immunogenicity risks use artificial stress methods to induce high levels of aggregation. These methods may be less biologically relevant in terms of their quantity than those that occur spontaneously during processing and storage. Here we describe the immunogenicity risk due to spontaneously occurring therapeutic antibody aggregates using peripheral blood mononuclear cells (PBMC) and a cell line with a reporter gene for immune activation: THP-1 BLUE NFκB. The spontaneously occurring therapeutic protein aggregates were obtained from process intermediates and final formulated drug substance from stability retains. Spontaneously occurring aggregates elicited innate immune responses for several donors in a PBMC assay with cytokine and chemokine production as a readout for immune activation. Meanwhile, no significant adaptive phase responses to spontaneously occurring aggregate samples were detected. While the THP-1 BLUE NFκB cell line and PBMC assays both responded to high stress induced aggregates, only the PBMC from a limited subset of donors responded to processing-induced aggregates. In this case study, levels of antibody aggregation occurring at process relevant levels are lower than those induced by stirring and may pose lower risk in vivo. Our methodologies can further inform additional immunogenicity risk assessments using a pre-clinical in vitro risk assessment approach utilizing human derived immune cells.
The phosphorylation of 2-(2 -hydroxyphenyl) benzoxazole has been accomplished with phosphorus oxychloride in a 1:1, 2:1, and 3:1 molar ratio in the presence of a base to yield O-phosphorylated benzoxazole derivatives. Their structures were confirmed by elemental analyses and IR, 1 H NMR, and 31 P NMR spectral studies. These compounds have been screened for their insecticidal activity against Periplenata americana and were found to be quite active in this respect.
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