A General Strategy for the Preparation of Thalidomide-Conjugate Linkers
The synthesis of small-molecule linkers for installation of thalidomide-based conjugates is described. Linker properties have been recognized as vital to conjugate success in drug discovery and delivery systems. These small-molecule tethers act as linkages between molecules, can also aid in cell permeability, and act as solubilizing agents. This work shows our progress in synthesizing conjugates with a variety of linker characteristics. The adaptability and manipulation of these and other linkers holds potential in improving synthetic control of chemical connectivities toward therapeutic development.
Papatzimas, James W.,Gorobets, Evgueni,Brownsey, Duncan K.,Maity, Ranjan,Bahlis, Nizar J.,Derksen, Darren J.
p. 2881 - 2885
(2017/10/07)
A new generation of specific Trypanosoma cruzi trans-sialidase inhibitors
(Chemical Equation Presented) A substitution for inhibition: The incorporation of anaryl substituent at C9 of 3-fluorosialyl fluorides provides specificity and dramatically slows the reactivation of the glycosylphosphatidylinositol-anchored surface protein Trypanosoma cruzi trans-sialidase (TcTS) by transglycosylation (see picture). X-ray crystallographic analysis of the trapped intermediate has provided a structural rationale for this behavior.
Buchini, Sabrina,Buschiazzo, Alejandro,Withers, Stephen G.
p. 2700 - 2703
(2008/12/23)
Effect of conformation of N-acyl carnosine and carcinine topochemical analogs on their antioxidant properties
To elucidate the influence of the nature of N-acyl substituent on antioxidant properties of carcinine analogs, the corresponding histamine derivatives were synthesized. Antioxidant activity of the compounds prepared was investigated in the Fe2+