Design, Synthesis, and Biological Evaluation of γ-Aminopropyl Silatrane-Acyclovir Hybrids with Immunomodulatory Effects

Abstract

Several derivatives of γ-aminopropyl silatrane containing acyclovir in their molecular structure were synthesized and evaluated for their immunomodulatory and antiviral activities. The structures of all these derivatives were confirmed by mass spectra, IR, and (1) H NMR. Based on WST-1 assay in vitro, these compounds could stimulate proliferation of splenic lymphocytes at certain concentrations. Furthermore, compound 3d could also potentiate the expression of IFN-γ, IL-2, CD4(+) , CD8(+) , and CD4(+) /CD8(+) in vivo. Our results show that these derivatives possess antiviral activity against herpes simplex viruses with a similar potency to acyclovir without a cellular immune response.

Keywords: acyclovir derivant; immunomodulatory activity; γ-aminopropyl silatrane.