An Aminopyrrolidinyl Phosphonates—A New Class of Antibiotics: Facile Synthesis and Predicted Biological Activity
Date
2020-12-04
Authors
Al Quntar, Abed Al Aziz
Dweik, Hasan
Jabareen, Ahmad
Gloriozova, Tatyana A.
Dembitsky, Valery M.
Journal Title
Journal ISSN
Volume Title
Publisher
Scientific Research Publishing
Abstract
A novel class of aminopyrrolidinyl phosphonates was synthesized in 74% -
80% isolated yield by the addition of three-fold excess of primary amines to
diethyl 4-chloro-1-butynylphosphonates. The reaction was carried out at
room temperature and in the absence of solvent or catalyst to give solely
compounds which showed predicted biological activity based on PASS program.
Some of the synthesized derivatives of antibiotics exhibit properties for
the treatment of stroke, the treatment of acute neurological disorders, and
can also be acetyl esterase inhibitors.
Description
Keywords
Alkynylphosphonates , Cyclization , Pyrrolidine , β-Aminophosphonates , Amine Addition , Antibiotics