Efficient and Short Method for Conjugation of 1-Nitro-9-Aminoacridine to Important Peptidyl Fragments by a Solid Support Synthesis.

Autor: Lahutta M; Department of Chemical Technology of Drugs, Faculty of Pharmacy, Medical University of Gdansk, Al. Gen. J., Hallera 107, 80-416, Gdansk, Poland.
Jazyk: angličtina
Zdroj: Chemistry & biodiversity [Chem Biodivers] 2021 Jan; Vol. 18 (1), pp. e2000702. Date of Electronic Publication: 2020 Dec 22.
DOI: 10.1002/cbdv.202000702
Abstrakt: The efficient and short techniques for conjugation of 9-aminoacridine with different peptidyl fragments are necessary for the development of active pharmaceutical ingredients (API). They need to be adopted to generate a new branch of acridine conjugates, enhancing their bioavailability for the examination in biological systems. The branch of developing acridine conjugates, built via different linkers and synthesized in this study, are expected as potential effective chemotherapeutics with dual mechanism of action. Recently, the methodology based on a solid-phase technique has been successfully demonstrated in preparing a number of promising compounds. However, the reaction conditions for amide bond formation between 1-nitro-9-aminoacridine and peptidyl fragments need to be optimized. In this study, the optimization of amide bond formation was demonstrated with the use of the solid-phase synthesis to build a new promising group of 1-nitro-9-aminoacridines conjugated to lactoferrin fragments via especially carboxy linker length.
(© 2020 Wiley-VHCA AG, Zurich, Switzerland.)
Databáze: MEDLINE
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