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Full-Text Articles in Physical Sciences and Mathematics
Synthesis Of Novel Agents For The Treatment Of Infectious And Neurodegenerative Diseases, Benjamin Joe Eduful
Synthesis Of Novel Agents For The Treatment Of Infectious And Neurodegenerative Diseases, Benjamin Joe Eduful
USF Tampa Graduate Theses and Dissertations
Infectious and neurodegenerative diseases continue to be a major concern worldwide. In spite of the great advances in drug therapy for treating various infectious and neurodegenerative diseases, there is still an urgent need for new and improved drugs due to increasing drug resistance among pathogens, emergence of new pathogens, ease of transmission of infections, ineffective available treatments, toxicity associated with current standard of care, aging populations and the lack of better alternative treatment options.
The first part of this manuscript (chapters 1 - 5) describes the synthesis of novel agents active against Leishmania donovani. According to the World Health Organization …
Design, Synthesis And Evaluation Of Novel Diazirine Photolabels With Improved Ambient Light Stability And Fluorous-Based Enrichment Capacity, Arun Babu Kumar
Design, Synthesis And Evaluation Of Novel Diazirine Photolabels With Improved Ambient Light Stability And Fluorous-Based Enrichment Capacity, Arun Babu Kumar
USF Tampa Graduate Theses and Dissertations
Photoaffinity labeling is a quintessential technique in studying and analyzing the interaction between a ligand and receptor. Diazirines are one of the important photo-labile moieties used in photoaffinity labeling due to their superior photo labeling characteristics. Herein, we report the investigations we conducted with diazirine photolabels on (a) photochemical aspects leading to enhancement of their ambient light stability and (b) equipping them with fluorous tags to enable fluorous enrichment of labeled proteins. Furthermore, we report a pilot study to develop BACE-1 inhibitors, which have potential to be developed into photoaffinity probes.
3-Trifluoromethyl-3-phenyldiazirine offers good selectivity and protection against pseudolabeling but …